Troglitazone

Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.

CAS No. 97322-87-7

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
10mg	JPY 22000	国内在庫あり
50mg	JPY 67000	国内在庫あり
200mg	JPY 175500	国内在庫なし(納期7~10日)
1g	JPY 598500	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（3）

製品安全説明書

現在のバッチを見る： S843201 DMSO] 88 mg/mL] true] Ethanol] 15 mg/mL] true] Water] Insoluble] false 純度： 99.47%

99.47

Troglitazone関連製品

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シグナル伝達経路

PPARシグナル伝達経路

PPAR阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
ST-13 cells	Function assay	5 μM	11 days	Induction of preadipocyte differentiation in mouse ST-13 cells assessed as lipid accumulation at 5 uM within 11 days by oil red-staining relative to control	19268587
HepG2 cells	Function assay	50 μM	24 h	Induction of p53 protein level in human HepG2 cells at 50 uM up to 24 hrs by immunoblot analysis	25851939
HEK293 cells	Function assay	10 μM	24 h	Transactivation of PPAR-gamma transfected in HEK293 cells at 10 uM after 24 hrs by luciferase reporter gene assay	22579484
HepG2 cells	Function assay	0.5-12.5 μM		Agonist activity at PPARgamma in human HepG2 cells assessed as down-regulation of glucose-6-phosphatase at 0.5 to 12.5 uM by real-time PCR method	22342624
HepG2 cells	Function assay	0.5-12.5 μM		Agonist activity at PPARgamma in human HepG2 cells assessed as down-regulation of phosphoenolpyruvate carboxykinase at 0.5 to 12.5 uM by real-time PCR method	22342624
MA104 cells	Cytotoxicity assay		24 h	Cytotoxicity against monkey MA104 cells after 24 hrs, TD50=18.5 μM	22365411
MDA-MB-231 cells	Proliferation assay		24 h	Antiproliferative activity hormone-independent human MDA-MB-231 cells after 24 hrs by luminescent cell viability assay, IC50=15.7 μM	22409968
MCF7 cells	Proliferation assay		24 h	Antiproliferative activity hormone-dependent human MCF7 cells after 24 hrs by luminescent cell viability assay, IC50=35.4 μM	22409968
HepG2 cells	Function assay		20 h	Transactivation of GAL4-fused PPARgamma LBD expressed in HepG2 cells after 20 hrs by luminescence assay, EC50=0.73 μM	22381047
LNCAP cells	Cytotoxicity assay		24 h	Cytotoxicity against human LNCAP cells after 24 hrs by MTT assay, IC50=22 μM	22546208
PC3 cells	Cytotoxicity assay		24 h	Cytotoxicity against human PC3 cells after 24 hrs by MTT assay, IC50=30 μM	22546208
CHO cells	Function assay		24 h	Agonist activity at human PPARgamma expressed in CHO cells co-transfected with pGL3-PPRE3-TK-luc assessed as transactivation after 24 hrs by firefly luciferase reporter gene assay, EC50=0.44 μM	22342624
HepG2 (DPX-2) cells	Function assay		24 h	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis, EC50=6.9 μM	20966043
3T3-L1 cells	Function assay			Effective concentration for 50% enhancement of insulin-induced triglyceride accumulation in 3T3-L1 cells, EC50=0.13 μM	9599241
PC12 cells	Proliferation assay			Concentration required for 50% inhibition of cell proliferation in PC12 cells using sulforhodamine B assay, IC50=15 Μm	15109648
A549	Growth inhibition assay			Inhibition of human lung cancer cell line (A549) by 50% in sulforhodamine B assay, GI50=15 μM	15454234
3T3L1 cells	Function assay			Increase in 2-deoxyglucose uptake in mouse 3T3L1 cells at 3 uM by liquid scintillation counter	18477507
HEK293 cells	Function assay			Agonist activity at PPARgamma expressed in HEK293 cells assessed as induction of receptor interaction with steroid receptor coactivator-1 by EYFP based reporter gene assay	16680159
CV-1 cells	Function assay			Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells, EC50=0.53703 μM	9836620
3T3L1 cells	Function assay			Agonist activity at PPARgamma in mouse 3T3L1 cells, EC50=1 μM	21493073
HepG2 cells	Function assay			Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of phosphoenolpyruvate carboxykinase mRNA by RT-PCR analysis	22424300
HEK293T cells	Function assay			Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis, IC50=4.5 Μm	23122865
HepG2 cells	Function assay			Agonist activity at PPARgamma in human HepG2 cells assessed as downregulation of glucose-6-phosphatase mRNA by RT-PCR analysis	22424300
HEK293 cells	Function assay			Activation of PPARgamma transfected in HEK293 cells after 18 hrs by firefly luciferase reporter gene-based luminescence assay relative to control, EC50=0.4 μM	21800856
rat ventricular myocytes	Function assay			Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes, IC50=9.5 μM	22761000
CV1 cells	Function assay			Transactivation of human PPARgamma expressed in african green monkey CV1 cells by luciferase reporter gene assay, EC50=0.4 μM	22579420
CHO cells	Function assay			Agonist activity at human recombinant PPARgamma expressed in CHO cells cotransfected with pGL3-PPRE3-TK-luc reporter assessed as beta-galactosidase activity at after 24 hrs by luciferase based transactivation assay, EC50=0.44 μM	22424300
HepG2 cells	Function assay			Transactivation of GAL4-fused PPARgamma ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay, EC50=0.72 μM	23031596
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生物活性

製品説明

Troglitazone is a potent agonist for the peroxisome proliferator-activated receptor-(PPAR) that is a ligand activated transcription factor regulating cell differentiation and growth. Troglitazone induces autophagy, apoptosis and necroptosis in bladder cancer cells. Troglitazone prevents RSL3-induced ferroptosis and lipid peroxidation in Pfa1 cells.

Targets

Ferroptosis ^[6]

PPAR ^[1]

In Vitro
In vitro	Troglitazone significantly inhibits cell growth by cell cycle arrest and apoptotic cell death. Troglitazone also downregulates surface expression of CD97, a novel dedifferentiation marker, in FTC-133 cells and upregulated sodium iodide symporter (NIS) mRNA in TPC-1 and FTC-133 cells. Troglitazone, a PPARγ agonist, induces antiproliferation and redifferentiation in thyroid cancer cell lines^[1]. Troglitazone induces Erk phosphorylation in human prostate cancer cells via a PPARγ-independent signaling pathway^[2]. TGZ(Troglitazone) up-regulates nitric oxide synthesis, induces the p53 pathway, inhibits cholesterol biosynthesis, induces p21 cyclin-dependent kinase inhibitor, has antioxidant function, and activates extracellular signal-regulated protein kinase (ERK) in a PPARγ-independent manner. TGZ induces Egr-1 expression by transcriptional and post-transcriptional regulation. Egr-1 induction by TGZ results in the increase of binding affinity and transactivation of the promoter containing Egr-1 consensus sequences, thereby possibly inducing other anti-tumorigenic proteins^[3].
細胞実験	細胞株	Thyroid cancer cell lines TPC-1, FTC-133, FTC-236, FTC-238, XTC-1 and ARO82-1 cell lines
	濃度	5, 10, 20, 40 μM
	反応時間	0, 2, 4, and 6 days
	実験の流れ	Growth experiments are done in a 96-well plate in hexaplicate. Cells at 85%-100% confluency are harvested with 1×Trypsin/EDTA solution and seeded into a 96-well plate at 3-5×10³ cells per well depending upon growth rate and maintained in 200 μL H5 medium in a humidified incubator. After 24 hours, cells are incubated with different concentrations of troglitazone and the media was changed daily. Colorometric dimethyl-thiazol-diphenyltetrazolium bromide (MTT) proliferation assays are performed at 0, 2, 4, and 6 days after treatment. MTT (400 μg/mL) is added to each well and incubated for 3 hours. It is solubilized with 0.04 N HCl/iso-propanol/3% SDS and incubated for 1 hour. The optical densities in the 96-well plates are determined using an enzyme-linked immunosorbent assay (ELISA) microplate reader at 595 nm/620 nm.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	ASCT2 / GLS1 c-Myc		25872876
	Growth inhibition assay	Cell viability		25872876

In Vivo
In Vivo	Troglitazone is an effective antidiabetic drug with a fundamentally new mechanism of action. However, within a year after its widespread use, individual cases of liver injury and failure are reported^[5]. TGZ significantly inhibits tumor growth of human colorectal cancer cells (HCT-116), human breast cancer cells (MCF-7), and human prostate cancer cells (PC-3) in immunodeficient mice^[3]. Troglitazone attenuates pancreatic damage and inflammation in experimental chronic pancreatitis^[4].
動物実験	動物モデル	C57BL/6 mice
	投与量	0.2% (with chow)
	投与経路	oral administration

参考
[1] Park JW, et al. Thyroid. 2005, 15(3):222-31. [2] Bolden A, et al. PPAR Res. 2012, 2012:929052. [3] Baek SJ, et al. J Biol Chem. 2003, 278(8):5845-53. [4] van Westerloo DJ, et al. Am J Pathol. 2005, 166(3):721-8. [5] Jaeschke H. Toxicol Sci. 2007, 97(1):1-3. [6] Sebastian Doll, et al. Nat Chem Biol . 2017 Jan;13(1):91-98. + 展開

参考

+ 展開

化学情報

分子量	441.54	化学式	C₂₄H₂₇NO₅S
CAS No.	97322-87-7	SDF	Download Troglitazone SDFをダウンロードする
Smiles	CC1=C(C2=C(CCC(O2)(C)COC3=CC=C(C=C3)CC4C(=O)NC(=O)S4)C(=C1O)C)C
保管	3年-20°C粉	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	3年-20°C粉	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 : 88 mg/mL ( (199.3 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。)

Ethanol : 15 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。

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):