Dexamethasone

別名：NSC 34521, Hexadecadrol, Prednisolone F,MK-125

製品コード：S1322 純度：99.68%

Dexamethasone is a potent synthetic member of the glucocorticoid class of steroid drugs, and an interleukin receptor modulator that has anti-inflammatory and immunosuppressant effects. Dexamethasone induces autophagy and mitophagy. Dexamethasone is tested in hospitalized patients with COVID-19 and is found to have benefits for critically ill patients.

CAS No. 50-02-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
50mg	JPY 22000	国内在庫あり
200mg	JPY 55500	国内在庫あり
1g	JPY 145500	国内在庫なし(納期7~10日)
10g	JPY 445500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（98）

製品安全説明書

現在のバッチを見る：純度： 99.68%

99.68

Dexamethasoneと併用されることが多い化合物

Pomalidomide

Dexamethasone and Pomalidomide application in treating relapsed or refractory multiple myeloma is still under clinical trials.

Siegel DS, et al. Br J Haematol. 2020;188(4):501-510.

Bortezomib

Dexamethasone and Bortezomib use results in highly effective and well-tolerated regimen for frontline treatment of multiple myeloma (MM).

Hassan Zafar MS, et al. South Asian J Cancer. 2018;7(1):58-60.

Venetoclax (ABT-199)

Dexamethasone and Venetoclax combination therapy induces long-term leukemia-free survival in PDX models.

Kirchhoff H, et al. Blood. 2021;137(19):2657-2661.

Lenalidomide

Dexamethasone and Lenalidomide demonstrate potent anti-MM activities both in vitro and in randomized phase III clinical trials.

Hideshima T, et al. Ther Clin Risk Manag. 2008;4(1):129-136.

Dexamethasone関連製品

関連製品	Tocilizumab (anti-IL-6R) Dexamethasone Acetate Dexamethasone Sodium Phosphate Sarilumab (anti-IL-6Rα)	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Bioactive Compound Library-Ⅱ	もっと見る

IL Receptor阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
mouse thymocytes	Function assay	1 μM	24 h	Induction of apoptosis in mouse thymocytes assessed as internucleosomal DNA fragmentation at 1 uM after 24 hrs by agarose gel electrophoresis	24794748
human monocytes	Function assay	5 μM	20 h	Antiinflammatory activity in human monocytes assessed as inhibition of LPS-induced COX2 expression at 5 uM after 20 hrs using rabbit polyclonal antibody IgG by SDS-PAGE analysis	21843935
R1	Function assay	10 uM	24 hrs	Inhibition of glucocorticoid receptor-glucocorticoid complex transfected in rat R1 cells assessed as down-regulation of TPA-responsive element proinflammatory gene expression at 10 uM after 24 hrs by beta-galactosidase assay, IC50 = 0.005 μM.	18412397
NIH-3T3	Function assay	0.01 mg/kg	1 hr	Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Cp = 0.044 μM.	20469868
NIH-3T3	Function assay	0.1 mg/kg	1 hr	Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Cp = 0.236 μM.	20469868
NIH-3T3	Function assay	1 mg/kg	1 hr	Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Cp = 1.8 μM.	20469868
NIH-3T3	Function assay	10 mg/kg	1 hr	Plasma concentration in mouse bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Cp = 17.7 μM.	20469868
NIH-3T3	Function assay	0.01 mg/kg	1 hr	Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.01 mg/kg, po after 1 hr, Fu = 0.00203 μM.	20469868
NIH-3T3	Function assay	0.1 mg/kg	1 hr	Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 0.1 mg/kg, po after 1 hr, Fu = 0.0116 μM.	20469868
NIH-3T3	Function assay	1 mg/kg	1 hr	Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 1 mg/kg, po after 1 hr, Fu = 0.087 μM.	20469868
NIH-3T3	Function assay	10 mg/kg	1 hr	Fraction unbound in mouse plasma bearing mouse NIH-3T3 cells integrated with MMTV reporter gene at 10 mg/kg, po after 1 hr, Fu = 5.123 μM.	20469868
RAW264.7	Antiinflammatory assay	10 uM	24 hrs	Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as nitrite level at 10 uM after 24 hrs by Griess method, Activity = 1.54 μM.	21353543
A549	Antiinflammatory assay	1 uM	30 mins	Antiinflammatory activity in human A549 cells assessed as inhibition of IL-1beta-induced mPGES1 expression at 1 uM treated 30 mins prior to IL-1beta challenge measured after 48 hrs by Western blot analysis relative to control	22795900
IOBA-NHC	Function assay	40 uM	24 hrs	Inhibition of NF-kappaB p65-mediated IL-6 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA	23219855
IOBA-NHC	Function assay	40 uM	24 hrs	Inhibition of NF-kappaB p65-mediated TNFalpha release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA	23219855
IOBA-NHC	Function assay	40 uM	24 hrs	Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human IOBA-NHC cells at 40 uM after 24 hrs by ELISA	23219855
HCLE	Function assay	40 uM	24 hrs	Inhibition of NF-kappaB p65-mediated IL-8 release in HSV1 KOS infected human HCLE cells at 40 uM after 24 hrs by ELISA	23219855
HCT116	Function assay	20 to 40 uM	24 hrs	Agonist activity at glucocorticoid receptor (unknown origin) expressed in human HCT116 cells co-expressing GRE at 20 to 40 uM after 24 hrs by luciferase reporter gene assay	23276449
B16F10	Antitumor assay	20 mg/kg	24 days	Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as inhibition tumor growth at 20 mg/kg, ip measured after 24 days of tumor inoculation	24992071
B16F10	Antitumor assay	20 mg/kg	24 days	Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by TUNEL assay	24992071
B16F10	Apoptosis assay	10 uM	48 hrs	Induction of apoptosis in mouse B16F10 cells assessed as increase in ratio of BAX/Bcl2 expression at 10 uM after 48 hrs by Western blot analysis relative to untreated control	24992071
B16F10	Antitumor assay	20 mg/kg	24 days	Antitumor activity against mouse B16F10 cells xenografted in C57BL/6 mouse assessed as apoptotic regions at 20 mg/kg, ip measured after 24 days of tumor inoculation by VE-cadherin	24992071
RAW264.7	Antiinflammatory assay	1 mM	30 mins	Antiinflammatory activity against mouse RAW264.7 cells assessed as reduction of LPS-induced TNF mRNA expression cells at 1 mM treated 30 mins before LPS challenge measured after 3 hrs by qRT-PCR analysis	25667960
J774	Antiinflammatory assay	10 uM	24 hrs	Antiinflammatory activity against mouse J774 cells assessed as inhibition of LPS-induced iNOS expression at 10 uM after 24 hrs by Western blot analysis	26915998
C57BL/6	Antiinflammatory assay	10 mg/kg	1 hr	Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced mononuclear cells migration in articular cavity at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs	27227459
C57BL/6	Antiinflammatory assay	10 mg/kg	1 hr	Antiinflammatory activity in C57BL/6 mouse assessed as inhibition of zymosan-induced infiltration of inflammatory cells into synovial tissue at 10 mg/kg, ip administered 1 hr prior to zymosan challenge measured at 6 to 24 hrs by hematoxylin and eosin stai	27227459
J774A.1	Antiinflammatory assay	1 uM	1 hr	Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced IL6 production in cell-free supernatant at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by sandwich ELISA	27227459
J774A.1	Antiinflammatory assay	1 uM	1 hr	Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced COX2 expression at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by Western blot analysis	27227459
J774A.1	Antiinflammatory assay	1 uM	1 hr	Antiinflammatory activity in mouse J774A.1 cells assessed as inhibition of zymosan and IFNgamma-induced nitric oxide production at 1 uM preincubated for 1 hr followed by zymosan and IFNgamma addition measured after 24 hrs by colorimetric Griess test	27227459
Mino	Antiproliferative assay	100 uM	48 hrs	Antiproliferative activity against human Mino cells at 100 uM preincubated for 48 hrs followed by thymidine addition measure after 16 hrs by Thymidine incorporation assay	28858511
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in COX2 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR ana	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 mRNA level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation for 6 hrs by RT-PCR analysi	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in NO production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by Grie	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-1beta production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs b	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in IL-6 production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by EL	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in TNFalpha production at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 3 hrs by	29389121
RAW264.7	Function assay	10 uM	1 hr	Agonist activity at PPARgamma in LPS-stimulated mouse RAW264.7 cells assessed as inhibition of NF-kappaB signaling by measuring reduction in iNOS protein level at 10 uM pretreated with compound for 1 hr followed by LPS stimulation measured after 24 hrs by	29389121
HeLa	Function assay	0.4 uM	24 hrs	Transrepression of GCR in human HeLa cells assessed as suppression of DEX-induced GILZ mRNA expression at 0.4 uM after 24 hrs by Taqman-based real-time PCR analysis	29670697
RAW264.7	Antiinflammatory assay	20 uM	6 hrs	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-6 production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA	30215255
RAW264.7	Antiinflammatory assay	20 uM	6 hrs	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced IL-1beta production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA	30215255
RAW264.7	Antiinflammatory assay	20 uM	6 hrs	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitrite production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA	30215255
RAW264.7	Antiinflammatory assay	20 uM	6 hrs	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced TNFalpha production at 20 uM pretreated for 6 hrs followed by LPS stimulation measured after 24 hrs by ELISA	30215255
A549	Function assay	10 uM		Antagonist activity for Glucocorticoid receptor in MMTV transactivation assay in human A549 lung epithelial cells at 10 uM, IC50 = 10 μM.	15999989
COS7	Function assay	1 uM		Agonist activity at glucocorticoid receptor Q570A mutant in COS7 cells at 1 uM by NF-kappaB-luciferase reporter gene assay	18038970
RAW264.7	Function assay	10 uM		Inhibition of LPS-stimulated COX2 expression in mouse RAW264.7 cells at 10 uM by Western blot	18790649
RAW264.7	Function assay		2 hrs	Inhibition of mPGES1 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis	17407277
RAW264.7	Function assay		2 hrs	Inhibition of COX2 expression in LPS-stimulated mouse RAW264.7 cells after 2 hrs by Western blot analysis	17407277
RAW 264.7	Function assay		24 hrs	Inhibition of interferon gamma-stimulated NO production in RAW 264.7 cells after 24 hrs, IC50 = 0.02 μM.	17367124
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in LPS-stimulated mouse RAW264.7 cells assessed as effect on TNFalpha formation pretreated 1 hr before LPS challenge measured after 24 hrs, IC50 = 0.7 μM.	11908984
rat polymorphonuclear leukocytes	Function assay		20 mins	Antiinflammatory activity in rat polymorphonuclear leukocytes assessed as inhibition of LPS-stimulated nitric oxide production after 20 mins by Griess method, IC50=2.3 nM	22506620
RPMI8226	Antiproliferative assay		4 days	Antiproliferative activity against human RPMI8226 cells after 4 days, IC50 = 0.0065 μM.	17705362
TH2	Function assay		48 hrs	Inhibition of pro-inflammatory cytokine IL5 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM.	19323483
TH2	Function assay		48 hrs	Inhibition of pro-inflammatory cytokine IL13 production in ovalbumin-stimulated BALB/c mouse TH2 cells after 48 hrs by sandwich-ELISA, IC50 = 0.005 μM.	19323483
A549	Function assay		6 hrs	Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of IL-1-beta-induced NF-kappaB dependent E-selection promoter activation after 6 hrs by luciferase reporter gene based ELAM assay, EC50 = 0.0011 μM.	20047280
A549	Function assay		6 hrs	Transrepression activity at glucocorticoid receptor expressed in human A549 cells assessed as inhibition of PMA-induced AP1 activity after 6 hrs by luciferase reporter gene assay, EC50 = 0.0025 μM.	20047280
U2OS	Function assay		18 hrs	Agonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as increase of transactivation activity after 18 hrs by luciferase reporter gene assay, EC50 = 15.8489 μM.	20812681
U2OS	Function assay		18 hrs	Antagonist activity at glucocorticoid receptor-LBD in human U2OS cells transfected with Gal4-DBD assessed as inhibition of transactivation activity after 18 hrs by luciferase reporter gene assay, IC50 = 0.0005082 μM.	20812681
HepG2	Function assay		24 hrs	Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis, EC50 = 2.6 μM.	20966043
13D3/Huh7	Function assay		24 hrs	Transactivation activity at glucocorticoid receptor in human 13D3/Huh7 cells assessed as induction of tyrosine aminotransferase activity after 24 hrs, EC50 = 0.005 μM.	21073190
RAW264.7	Antiinflammatory assay		18 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 2 hrs before LPS challenge measured after 18 hrs by griess reaction, IC50 = 0.86 μM.	21288727
HMC1	Function assay		1 hr	Immunomodulatory activity in human HMC1 cells assessed as inhibition of phorbol 12-myristate 13-acetate/A23187-stimulated IL1-beta secretion treated 1 hr prior to 30 mins phorbol 12-myristate 13-acetate/A23187 challenge by Western blotting analysis	21302967
RAW264.7	Antiinflammatory assay		18 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs, IC50 = 0.01 μM.	21353543
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess method, IC50 = 0.8 μM.	21353543
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of IFN-gamma induced NO production after 24 hrs by Griess reaction, IC50 = 0.02 μM.	21361338
RAW264.7	Function assay		20 mins	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells pre-incubated for 20 mins before LPS challenge measured 18 hrs post LPS challenge by Griess method	21775152
RAW264.7	Function assay		30 mins	Inhibition of LPS-induced TNFalpha production in mouse RAW264.7 cells pre-incubated for 30 mins before LPS challenge measured 6 hrs post LPS challenge by ELISA	21775152
RAW264.7	Antiinflammatory assay		2 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.47 μM.	22372956
RAW264.7	Antiinflammatory assay		2 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production pretreated for 2 hrs before LPS challenge measured after 18 hrs by Griess method, IC50 = 0.98 μM.	22537362
H13	Function assay		3 hrs	Inhibition of glucocorticoid receptor in human H13 cells assessed as inhibition of glucocorticoid-induced cell proliferation after 3 hrs by [3H]-thymidine incorporation assay, EC50 = 0.0097 μM.	23199485
293 MSR	Function assay		60 mins	Displacement of [3H]-dexamethasone human glucocorticoid receptor alpha expressed in 293 MSR cells after 60 mins by scintillation counting, EC50 = 0.0125 μM.	23199485
RAW264.7	Antiinflammatory assay		2 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 2 hrs prior to LPS-challenge measured after 24 hrs by Griess method, IC50 = 1.43 μM.	23373965
HeLaS3	Function assay		2 hrs	Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, IC50 = 0.0041 μM.	23403082
HeLaS3	Function assay		2 hrs	Displacement of [3H]Dexamethasone from glucocorticoid receptor in human HeLaS3 cells after 2 hrs, Ki = 0.0022 μM.	23403082
CUTLL1	Growth inhibition assay		48 hrs	Growth inhibition of human CUTLL1 cells with high GR expression levels after 48 hrs by alamar blue assay	25050160
RAW264.7	Function assay		24 hrs	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay relative to vehicle-treated control, IC50 = 0.8 μM.	25499882
SW1353	Function assay		24 hrs	Transrepression activity at glucocorticoid receptor in human SW1353 cells assessed as repression of IL-1-induced MMP-13 production after 24 hrs by ELISA, IC50 = 0.0018 μM.	25706100
RAW264.7	Function assay		6 hrs	Inhibition of TNFalpha production in mouse RAW264.7 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.04 μM.	25824662
J774A.1	Function assay		6 hrs	Inhibition of TNFalpha production in mouse J774A.1 cells incubated for 6 hrs by sandwich immunoassay, IC50 = 0.4 μM.	25824662
RAW264.7	Function assay		12 hrs	Inhibition of IL-1beta production in mouse RAW264.7 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 4.7 μM.	25824662
J774A.1	Function assay		12 hrs	Inhibition of IL-1beta production in mouse J774A.1 cells incubated for 12 hrs by sandwich immunoassay, IC50 = 22 μM.	25824662
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.63 μM.	26087384
BV2	Antiinflammatory assay		24 hrs	Antiinflammatory activity in C57BL6/J mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 0.025 μM.	26110443
RAW264.7	Function assay		24 hrs	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 0.8 μM.	26305406
RAW264.7	Antiinflammatory assay		24 hrs	Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs in presence of LPS by Griess assay, IC50 = 0.63 μM.	27825545
RAW264.7	Antiinflammatory assay		30 mins	Antiinflammatory activity in mouse RAW264.7 cells assessed as reduction in LPS-induced NO production pretreated for 30 mins followed by LPS stimulation for 24 hrs by Griess assay, IC50 = 7 μM.	28499733
RAW264.7	Function assay		24 hrs	Inhibition of LPS-induced NO production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 2.5 μM.	28598633
RAW264.7	Function assay		24 hrs	Inhibition of LPS-induced nitric oxide production in mouse RAW264.7 cells after 24 hrs by Griess assay, IC50 = 10.7 μM.	29518326
HFF	Antiinflammatory assay			Antiinflammatory activity assessed as upregulation of aromatase in HFF cells by transactivation assay, EC50 = 0.002 μM.	17692519
HFF	Antiinflammatory assay			Antiinflammatory activity assessed as inhibition of IL1 stimulated IL6 production in HFF cells by transrepression assay, EC50 = 0.0005 μM.	17692519
A549	Function assay			Antagonist activity at glucocorticoid receptor in human A549 cells transfected with MMTV luciferase reporter gene assessed as inhibition of dexamethasone-induced activation, IC50 = 1 μM.	17616395
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM.	17616395
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.00537 μM.	17616395
HFF	Function assay			Inhibition of IL1-stimulated IL6 production in HFF cells, IC50 = 0.00051 μM.	17181172
HeLa	Function assay			Activation of MMTV in HeLa cells measured by luciferase activity, EC50 = 0.017 μM.	17181172
HFF	Function assay			Induction of aromatase activity in HFF cells assessed as production of beta estradiol by aromatase assay, EC50 = 0.0019 μM.	17181172
A549	Function assay			Agonist activity at GR assessed as NF-kappaB-mediated transrepression of secreted placental alkaline phosphatase gene in human A549 cells, IC50 = 0.001175 μM.	16821781
A549	Function assay			Agonist activity at GR assessed as MMTV-mediated transactivation of renilla luciferase gene in human A549 cells relative to Dexamethasone, EC50 = 0.005012 μM.	16821781
A549	Function assay			Activity at glucocorticoid receptor in human A549 cells assessed as effect on GRE promoter response by luciferase reporter assay, EC50 = 0.001 μM.	16643060
RAW 264.7	Function assay			Inhibitory activity against TNF-alpha release in RAW 264.7 cells in the supernatant, IC50 = 0.42 μM.	12361395
N9	Function assay			Inhibitory activity against TNF-alpha release in N9 cells in the supernatant, IC50 = 0.074 μM.	12361395
PBMC	Function assay			Inhibitory concentration against growth of LPS stimulated human peripheral blood mononuclear cells, IC50 = 0.04 μM.	11229767
PBMC	Function assay			Inhibitory concentration against TNF-alpha production from human peripheral blood mononuclear cells stimulated by LPS, IC50 = 0.01 μM.	11229767
T-cell	Function assay			Inhibitory concentration against T cell proliferation using concanavalin A stimulated mice spleen cells, IC50 = 0.005 μM.	11229767
CV1	Function assay			Agonist activity at human GR expressed in CV1 cells by GRE activation assay, EC50 = 0.0002 μM.	17705362
NHDFneo	Function assay			Activity at human GR expressed in NHDFneo cells assessed as inhibition of IL-6 production, IC50 = 0.0014 μM.	17705362
J774A.1	Function assay			Inhibition of LPS-induced TNFalpha production in mouse J774A.1 cells, IC50 = 0.048 μM.	17892941
CV1	Function assay			Activity at human glucocorticoid receptor expressed in CV1 cells assessed as repression of TNF and IL-1-beta-induced E-selectin gene expression by luciferase reporter gene assay, ED50 = 0.0001 μM.	18032610
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by MMTV transactivation assay, EC50 = 0.005012 μM.	18038970
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001175 μM.	18038970
HeLa	Cytotoxicity assay			Cytotoxicity against human HeLa cells assessed as inhibition of DNA replication by imaging analysis	18066055
HeLa	Function assay			Inhibition of mitosis in human HeLa cells by imaging analysis	18066055
THP1	Antiinflammatory assay			Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL6 by ELISA, IC50 = 0.007 μM.	18625560
THP1	Antiinflammatory assay			Antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced TNFalpha by ELISA, IC50 = 0.05 μM.	18625560
RAW264.7	Function assay			Inhibition of LPS-stimulated microsomal prostaglandin E synthase 1 expression at 10 uM in mouse RAW264.7 cells by Western blot	18790649
A549	Function assay			Transrepression activity at GR in IL-1-beta-stimulated human A549 cells assessed as inhibition of NF-kappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM.	19321341
A549	Function assay			Transrepression activity at GR in PMA-stimulated human A549 cells assessed as inhibition of AP1 response element-induced luciferase reporter gene activity, EC50 = 0.0025 μM.	19321341
NP1	Function assay			Agonist activity at GR ligand binding domain expressed in human NP1 cells assessed as glucocorticoid response element transactivation by GAL4 luciferase reporter gene assay, EC50 = 0.0042 μM.	19321341
MDA-kb2	Function assay			Agonist activity at androgen receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM.	19592245
MDA-kb2	Function assay			Agonist activity at glucocorticoid receptor in human MDA-kb2 cells assessed as stimulation of luciferase activity by luciferase reporter gene assay, EC150 = 0.194 μM.	19592245
A549	Function assay			Agonist activity at GR in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM.	19592247
COS7	Function assay			Agonist activity at glucocorticoid receptor ligand binding domain expressed in african green monkey COS7 cells co-transfected with Gal4-LBD by luciferase reporter gene assay, EC50 = 0.0072 μM.	19863083
HeLa	Function assay			Transactivation of GAL-4 tagged glucocorticoid receptor ligand binding domain expressed in human HeLa cells assessed as NP1 activation by luciferase reporter gene assay, EC50 = 0.0045 μM.	20047280
HeLa	Function assay			Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, EC50 = 0.007943 μM.	20727743
HeLa	Function assay			Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM.	20727743
THP1	Function assay			Transrepression activity at glucocorticoid receptor-mediated antiinflammatory activity in human THP1 cells assessed as inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM.	20727743
Sf9	Function assay			Binding affinity to human recombinant glucocorticoid receptor expressed in baculovirus infected Sf9 cells, IC50 = 0.01259 μM.	20727743
insect cells	Function assay			Binding affinity to glucocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.0034 μM.	20735001
insect cells	Function assay			Binding affinity to mineralocorticoid receptor expressed in baculovirus-infected insect cells using tetramethylrhodamine labeled Dexamethasone by fluorescence polarization microplate assay, IC50 = 0.033 μM.	20735001
A549	Function assay			Transrepression activity of glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM.	21073190
A549	Function assay			Transrepression activity of glucocorticoid receptor in human A549 cells expressing AP-1 assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM.	21073190
NP-1 Hela	Function assay			Transactivation activity of glucocorticoid receptor ligand binding domain expressed in human NP-1 Hela cells co-expressing GAL4 DNA binding domain by luciferase reporter gene assay, EC50 = 0.0042 μM.	21073190
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells by NF-kappaB transrepression assay, IC50 = 0.001 μM.	21257309
A549	Function assay			Agonist activity at GR in human A549 cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, IC50 = 0.003981 μM.	21257309
HeLa	Function assay			Agonist activity at glucocorticoid receptor in human HeLa cells transfected with luciferase gene linked to MMTV promoter assessed as luciferase transactivation activity, EC50 = 0.017 μM.	21963986
insect cells	Function assay			Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant glucocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.003 μM.	21963986
insect cells	Function assay			Displacement of tetramethylrhodamine-labeled Dexamethasone from human recombinant mineralocorticoid receptor expressed in baculovirus infected insect cells by fluorescence polarization assay, IC50 = 0.033 μM.	21963986
A549	Function assay			Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL1beta-stimulated NFkappaB-dependent E-selectin transcription by luciferase reporter gene assay, EC50 = 0.0011 μM.	23916594
A549	Function assay			Transrepression activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-stimulated AP1 response element by luciferase reporter gene assay, EC50 = 0.0025 μM.	23916594
Hela	Function assay			Transactivation activity at glucocorticoid receptor ligand binding domain (unknown origin) expressed in human Hela cells co-expressing GAL4 DNA binding domain assessed as NP-1-stimulated GRE activation by luciferase reporter gene assay, EC50 = 0.0045 μM.	23916594
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of IL-1beta-induced NF-kappaB dependent E-selectin activation by luciferase reporter gene assay, EC50 = 0.0011 μM.	23953070
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activation by luciferase reporter gene assay, EC50 = 0.0025 μM.	23953070
HeLa	Function assay			Transactivation of glucocorticoid receptor ligand binding domain (unknown origin) transfected in human HeLa cells assessed as activation of NP-1 by GAL4 luciferase reporter gene assay, EC50 = 0.0045 μM.	23953070
A549	Function assay			Transrepression of glucocorticoid receptor in human A549 cells assessed as inhibition of PMA-induced AP-1 activity by luciferase reporter gene assay, EC50 = 0.0025 μM.	24011644
HeLa	Function assay			Transactivation of GR-LBD expressed in human HeLa cells co-expressing GAL4-DBD by luciferase reporter gene assay, EC50 = 0.0042 μM.	24011644
HEK293	Function assay			Displacement of [3H]-aldosterone from human mineralocorticoid receptor expressed in HEK293 cells, Ki = 0.00036 μM.	24446728
HEK293	Function assay			Displacement of [3H]-dexamethasone from human glucocorticoid receptor expressed in HEK293 cells, Ki = 0.00069 μM.	24446728
HEK293	Function assay			Displacement of [3H]-methyltrienolone from human progesterone receptor expressed in HEK293 cells, Ki = 0.561 μM.	24446728
HEK293	Function assay			Displacement of [3H]-methyltrienolone from human androgen receptor expressed in HEK293 cells, Ki = 1.41 μM.	24446728
HeLa	Function assay			Transactivation of glucocorticoid receptor in human HeLa cells harboring MMTV promoter by luciferase reporter gene assay, EC50 = 0.017 μM.	24656565
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells assessed as E-selectin transrepression by luciferase reporter gene assay, EC50 = 0.0011 μM.	24980053
A549	Function assay			Agonist activity at glucocorticoid receptor in human A549 cells assessed as AP-1 transrepression by luciferase reporter gene assay, EC50 = 0.0025 μM.	24980053
HeLa	Function assay			Agonist activity at glucocorticoid receptor in human HeLa cells assessed as NP-1 transactivation by luciferase reporter gene assay, EC50 = 0.0045 μM.	24980053
HEK293	Function assay			Agonist activity at human GCR expressed in HEK293 cells by luciferase reporter gene assay, EC50 = 0.0013 μM.	25305688
HFF	Function assay			Agonist activity at GR in HFF cells assessed as suppression of IL-1-induced IL-6 production, IC50 = 0.001 μM.	25516791
IM9	Function assay			Displacement of [3H]dexamethasone from glucocorticoid receptor in human IM9 cells, IC50 = 0.0038 μM.	26988801
IM9	Function assay			Displacement of [3H]dexamethasone from GR receptor in human IM9 cells, IC50 = 0.0038 μM.	27876250
HeLa	Function assay			Transrepression activity at glucocorticoid receptorin human HeLa cells assessed as inhibition of TPA-induced collagenase promoter activity by luciferase reporter gene assay, IC50 = 0.001585 μM.	28043796
THP1	Function assay			Transrepression activity at glucocorticoid receptor in human THP1 cells assessed as receptor-mediated anti-inflammatory activity by measuring inhibition of LPS-induced IL-8 production, IC50 = 0.002512 μM.	28043796
HeLa	Function assay			Transactivation activity at glucocorticoid receptor in human HeLa cells assessed as induction of MMTV promoter activity by luciferase reporter gene assay, IC50 = 0.007943 μM.	28043796
Sf9	Function assay			Binding affinity to recombinant human glucocorticoid receptor expressed in baculovirus infected sf9 cells, IC50 = 0.01259 μM.	28043796
RAW264.7	Antiinflammatory assay			Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production by griess assay, IC50 = 0.8 μM.	29272126
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
BV2	Antiinflammatory assay			Antiinflammatory activity in mouse BV2 cells assessed as inhibition of LPS-induced nitric oxide production, IC50 = 9.5 μM.	29482940
RAW264.7	Antiinflammatory assay			Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production, IC50 = 8.3 μM.	29741372
HEK 293T	Function assay			Agonist activity at GAL4 DNA-binding domain fused GR (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay, IC50 = 0.00235 μM.	30144697
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生物活性

製品説明

Targets

interleukin receptor ^[1]
(Cell-free assay)

In Vitro
In vitro	Dexamethasone results in decrease in transmonolayer paracellular permeability mainly to sucrose, fluorescein and dextrans of up to 20 KDa in an immortalised rat brain endothelial cell line (GPNT). Dexamethasone results in filamentous actin and the cytoskeleton associated protein cortactin being highly concentrated in the regions of cell-cell contact with few F-actin stress fibres visible within the cytoplasm in cultured rat brain endothelial cells, an observation consistent with a more differentiated barrier phenotype induced by dexamethasone. Dexamethasone treatment has been shown to strongly stimulate the level of the Id-1 protein, which is a serum-inducible helix-loop-helix transcriptional repressor, involved in cell differentiation, and this effect was shown to be associated with reorganisation of ZO-1 to the cell periphery in Con8 mammary epithelial tumor cells. Dexamethasone prevents cytokine-induced enhanced expression of MMP-9 and alterations in the expression of ZO-1 in untreated GPNT monolayers. ^[1] Dexamethasone depletes both basal and TNF-alpha-stimulated GSH levels by down-regulating the gamma-GCS-heavy subunit transcription via a mechanism involving AP-1 (c-Jun) in alveolar epithelial cells. Dexamethasone decreases both basal and stimulated GSH levels (TNF-α-treated) in alveolar epithelial cells (A549), without any change in GSSG. ^[2]
細胞実験	細胞株	CB CD34+ cells
	濃度	1 μM
	反応時間	16 h
	実験の流れ	Cells were treated with indicated concentrations of drug.
実験結果図	Methods	Biomarkers	結果図	PMID
実験結果図	Western blot	Bcl-2 / Bcl-xl / Mcl-1 / Survivin / IAP1 Cyclin D1 / Cyclin E / COX-2 / MMP-9 Bax / p21 p-JNK / JNK / p-p38 / p38 / p-ERK / ERK		28696369

In Vivo
In Vivo	Dexamethasone is administered i.m. to pregnant ewes, leads to the following results (1) blood pressure is unchanged; (2) as previously reported in the fetus, sensitivity to endothelin-1 (ET) is increased; (3) acetylcholine-induced relaxation is increased; (4) L-NAME suppressible vasodilatory response to ET is abolished; (5) there is no change in endothelium-independent vasodilatation; and (6) there is no change in eNOS RNA and protein levels, when compared to saline treated controls. ^[3]
動物実験	動物モデル	Mice
	投与量	1 mg/kg
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06118710	Not yet recruiting	Cancer	Erasmus Medical Center	January 1 2024	Phase 4
NCT05759481	Not yet recruiting	Post-operative Nausea and Vomiting	Milton S. Hershey Medical Center	January 2024	Phase 2
NCT06133712	Recruiting	Carpal Tunnel\|Dexmedetomidine\|Ozone\|Dexamethasone	Tanta University	November 1 2023	Not Applicable
NCT05994183	Withdrawn	Bronchiolitis	IDeA States Pediatric Clinical Trials Network\|National Institutes of Health (NIH)\|University of Nebraska	October 9 2023	Early Phase 1

参考
[1] Romero IA, et al. Neurosci Lett, 2003, 344(2), 112-116. [2] Rahman I, et al. Biochem Pharmacol, 2000, 60(8), 1041-1049. [3] Molnar J, et al. J Physiol, 2003, 547(Pt 1), 61-66. [4] Suzuki E, et al. Clin Cancer Res, 2005, 11(18), 6713-6721. [5] Kunnumakkara AB, et al. Cancer Res, 2007, 67(8), 3853-3861. [6] Guo B, et al. Nat Med. 2017 Apr;23(4):424-428. [7] Zhang M, et al. Blood. 2022 Sep 22;140(12):1390-1407. + 展開

参考

+ 展開

化学情報

分子量	392.46	化学式	C₂₂H₂₉FO₅
CAS No.	50-02-2	SDF	Download Dexamethasone SDFをダウンロードする
Smiles	CC1CC2C3CCC4=CC(=O)C=CC4(C3(C(CC2(C1(C(=O)CO)O)C)O)F)C
保管	powder, 4°C (in the dark) ; in solvent，-80°C (in the dark)	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	powder, 4°C (in the dark) ; in solvent，-80°C (in the dark)	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 78 mg/mL ( (198.74 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 11 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

よくある質問（FAQ）

質問1:
I'm loonkig for Dexamethasone to use in cell culture, would it be better to use the Dexamethasone S1322, the sodiume phosphate S4028 or the acetate S3124?

回答
S1322 is the free base form of Dexamethasone, S4028 is the sodium phosphate form and S3124 is the acetate salt. All of them have similar biological activity in tissue culture, however, their suitabilities vary in different solvents. As free base, S1322 has high solubility in DMSO (79mg/ml), poor solubility in water (<1mg/ml), and moderate solubility in ethanol (6mg/ml). As sodium phosphate salt, S4028 has high solubility in water (103mg/ml) but is insoluble in DMSO and ethanol (<1mg/ml). The solubility of S3124 is 87mg/ml in DMSO, <1mg/ml in water, and 20mg/ml in ethanol. Selection can be made based on the customer's experimental setup.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):