GW3965 HCl

GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.

GW3965 HCl化学構造

CAS No. 405911-17-3

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 36000 国内在庫あり
JPY 29500 国内在庫あり
JPY 85500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)
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(42)

製品安全説明書

現在のバッチを見る: 純度: 99.9%
99.9

GW3965 HClと併用されることが多い化合物

Carboplatin


GW3965 and Carboplatin significantly reduce the relative tumor volume than carboplatin alone in the MAS98.12 model.

Haugen MH, et al. Mol Oncol. 2023 Jun 21.

Pioglitazone


GW3965 and Pioglitazone combination pretreatment in primary microglia cells produce a significant decrease in iNOS transcripts.

Skerrett R, et al. J Biol Chem. 2015 Aug 28;290(35):21591-602.

Bexarotene


GW3965 HCl and Bexarotene induce differentiation and apoptosis in acute myeloid leukemia (AML) cells.

Serhan N, et al. Cancers (Basel). 2020 Jun 29;12(7):1725.

Gefitinib


GW3965 can increase gefitinib-induced apoptosis and cell cycle arrest in HCC827/GR-8-2 cell line.

Hu Y, et al. Oncotarget. 2017 Feb 28;8(9):15802-15814.

Navitoclax (ABT-263)


GW3965 and Navitoclax (ABT-263) combination treatment reduces tumor growth significantly stronger than either drug alone in A375 xenograft model.

Nguyen TTT, et al. EMBO Mol Med. 2019 Oct;11(10):e10769.

GW3965 HCl関連製品

Liver X Receptor阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
HEK293 10 uM 20 hrs Activation of rat LXRbeta expressed in HEK293 cells co-expressing human RXRalpha at 10 uM after 20 hrs by luciferase reporter gene assay 28006909
HEK293 10 uM 20 hrs Activation of human LXRalpha expressed in HEK293 cells co-expressing human RXRalpha at 10 uM after 20 hrs by luciferase reporter gene assay 28006909
HepG2 Function assay 500 nM Inhibition of 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid-induced srebp1c mRNA expression in human HepG2 cells at 500 nM 18800767
HepG2 Function assay 500 nM Inhibition of 2-(3-(3-((2-chloro-3-(trifluoromethyl)benzyl)(2,2-diphenylethyl)amino)propoxy)phenyl)acetic acid-induced fas mRNA expression in human HepG2 cells at 500 nM 18800767
RAW264.7 Function assay 1 uM Reduction of LPS-stimulated iNOS gene expression in mouse RAW264.7 cells expressing LXRalpha at 1 uM by luciferase reporter gene assay 18800767
RAW264.7 Function assay 1 uM Inhibition of LPS-stimulated nuclear co-repressor release from iNOS promoter in mouse RAW264.7 cells at 1 uM by RT-PCR 18800767
HeLa Function assay 1 uM Induction of LXRbeta SUMOylation by SUMO2 in human HeLa cells at 1 uM by Western blot analysis 18800767
HeLa Function assay 1 uM Induction of LXRbeta SUMOylation by SUMO3 in human HeLa cells at 1 uM by Western blot analysis 18800767
HeLa Function assay 1 uM Induction of LXRalpha SUMOylation by SUMO3 in human HeLa cells at 1 uM by Western blot analysis 18800767
THP1 Antiinflammatory assay 6 hrs Antiinflammatory activity against human THP1 cells assessed as inhibition of LPS-stimulated IL6 production after 6 hrs by ELISA, IC50 = 0.02 μM. 18800767
COS7 Function assay 16 hrs Agonist activity at human LXRbeta receptor transfected in COS7 cells after 16 hrs by reporter transactivation assay, EC50 = 0.015 μM. 17587573
THP1 Function assay 18 hrs Induction of cholesterol efflux in THP1 cells after 18 hrs, EC50 = 0.01 μM. 17416521
RAW264.7 Function assay 24 hrs Induction of [3H]cholesterol efflux in mouse RAW264.7 cells loaded with acetylated-LDL after 24 hrs, EC50 = 0.029 μM. 19717304
SH-SY5Y Function assay 24 hrs Agonist activity at human LXRbeta expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay, EC50 = 0.13 μM. 19264481
SH-SY5Y Function assay 24 hrs Agonist activity at human LXRalpha expressed in human SH-SY5Y cells co-transfected with Gal4-LBD after 24 hrs by luciferase reporter gene assay, EC50 = 0.31 μM. 19264481
CHOK1 Function assay 24 hrs Agonist activity at Gal4-tagged LXRbeta (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay, EC50 = 0.42 μM. 25677664
CHOK1 Function assay 24 hrs Agonist activity at Gal4-tagged LXRalpha (unknown origin) expressed in CHOK1 cells after 24 hrs by luciferase reporter gene assay, EC50 = 1.3 μM. 25677664
THP1 Function assay Agonist activity at GAL-linked human LXRbeta expressed in THP1 cells assessed as stimulation of co-activator recruitment by FRET assay, EC50 = 0.027 μM. 17665897
COS7 Function assay Activation of LXRbeta co-transfected in COS7 cells with RXRalpha by reporter transactivation assay, EC50 = 0.015 μM. 17416521
THP1 Function assay Induction of cholesterol efflux in THP1 cells, EC50 = 0.01 μM. 17587573
THP1 Function assay Stimulation of [3H]cholesterol efflux in human THP1 foam cells loaded with ac-LDL, EC50 = 0.031 μM. 18973288
CV1 Function assay Antagonist activity at LXRbeta ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, IC50 = 0.03981 μM. 20345102
THP1 Function assay Agonist activity at GAL-linked human LXRalpha expressed in THP1 cells assessed as stimulation of coactivator recruitment by FRET assay, EC50 = 0.097 μM. 17665897
CV1 Function assay Antagonist activity at LXRalpha ligand binding domain assessed as inhibition of T1317-induced transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, IC50 = 0.1 μM. 20345102
HepG2 Function assay Effect on SREBP1c gene expression in human HepG2 cells, EC50 = 0.21 μM. 18973288
HuH7 Function assay Agonist activity at human recombinant LXRbeta ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 0.31 μM. 18973288
CHO Function assay Agonist activity at human LXR beta receptor expressed in CHO cells by reporter assay, EC50 = 0.41 μM. 17034119
THP1 Function assay Effect on ABCA1 gene expression in human differentiated THP1 cells, EC50 = 0.434 μM. 18973288
CV1 Function assay Agonist activity at LXRbeta ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, EC50 = 0.50119 μM. 20345102
HuH7 Function assay Agonist activity at human recombinant LXRalpha ligand binding domain in human HuH7 cells co-transfected with fused Gal4-DBD by transactivation assay, EC50 = 0.66 μM. 18973288
CV1 Function assay Agonist activity at LXRalpha ligand binding domain-mediated transcriptional activity in african green monkey CV1 cells co-transfected with Gal4-SRC1 by luciferase reporter assay, EC50 = 0.79433 μM. 20345102
HepG2 Function assay Effect on triglyceride accumulation in human HepG2 cells, EC50 = 2.002 μM. 18973288
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
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
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
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生物活性

製品説明 GW3965 HCl is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM in cell-free assays, respectively.
Targets
hLXRβ [1]
(Cell-free assay)
LXRα/SRC1 LiSA [1]
(Cell-free assay)
hLXRα [1]
(Cell-free assay)
30 nM(EC50) 125 nM(EC50) 190 nM(EC50)
In Vitro
In vitro

GW3965 recruits the steroid receptor coactivator 1 to human LXRα with EC50 of 125 nM in a cell-free ligand-sensing assay. [1]

GW3965 shows a potent antagonistic activity against hLXRα and hLXRβ in cell-based assays with EC50 of 190 nM and 30 nM, respectively. Besides, GW3965 also sows excellent selectivity over other nuclear receptors. [1]

In human islets, GW3965 (1 μM) reduces expression of selected pro-inflammatory cytokines including IL-8, monocyte chemotactic protein-1 and tissue factor. [4]

実験結果図 Methods Biomarkers 結果図 PMID
Western blot Skp2 / pEGFR / EGFR / pERK / ERK LXRα / LXRβ / ABCA1 / ABCG1 25184494
Immunofluorescence LAMP-1 / LDLR pRelA 23382078
Growth inhibition assay Cell viability 25184494
In Vivo
In Vivo

In mice, GW3965 at a dose of 10 mg/kg upregulates ABCA1 expression 8-fold and raises circulating levels of HDL by 30% with Cmax of 12.7 μg/mL and t1/2 of 2 hours. [1]

GW3965 (10mg/kg) induces expression of ABCA1 and ABCG1 and shows potent antiatherogenic activity in both LDLR−/− and apoE−/− mice. [2]

In male sprague-dawley rats, GW3965 reduces Ang II-mediated increases in blood pressure and decreases vascular Ang II receptor gene expression. [3]

In Glioblastoma mouse model, GW3965 results in inducible degrader of LDLR-mediated LDLR degradation, increased expression of the ABCA1 cholesterol efflux transporter, and thus potently promotes tumor cell death. [5]

動物実験 動物モデル C57BL/6 mice
投与量 ≤10 mg/kg
投与経路 Administered via p.o.

化学情報

分子量 618.51 化学式

C33H31ClF3NO3.HCl

CAS No. 405911-17-3 SDF Download GW3965 HCl SDFをダウンロードする
Smiles C1=CC=C(C=C1)C(CN(CCCOC2=CC=CC(=C2)CC(=O)O)CC3=C(C(=CC=C3)C(F)(F)F)Cl)C4=CC=CC=C4.Cl
保管

In vitro
Batch:

DMSO : 124 mg/mL ( (200.48 mM); Warmed with 50℃ water bath; 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。)

Water : Insoluble

Ethanol : 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

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)

mg/kg g μL

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。

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よくある質問(FAQ)

質問1:
How to formulate the compound for mouse in vivo experiment?

回答
S2630 GW3965 HCl can be dissolved in 2% DMSO/30% PEG 300/dd H2O at 10 mg/mL as a homogeneous suspension. This vehicle is suitable for oral gavage to mice.

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