Troglitazone-CS-045-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETroglitazoneCat. No.: HY-50935CAS No.: 97322-87-7Synonyms: CS-045分式: CHNOS分量: 441.54作靶点: PPAR; Autophagy作通路: Cell Cycle/DNA Damage; Autophagy储存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL

2、(226.48 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2648 mL 11.3240 mL 22.6480 mL5 mM 0.4530 mL 2.2648 mL 4.5296 mL10 mM 0.2265 mL 1.1324 mL 2.2648 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验

3、结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.66 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.66 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% c

4、orn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (5.66 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 TroglitazonePPAR 的激动剂，对和 PPAR的 EC50 值分别为 550 nM 和 780 nM。IC50 & Target PPAR550 nM (EC50, Human PPAR)体外研究 Troglitazone is a PPAR agonist, with EC50s of 550 nM and 780 nM for h

5、uman and murinePPAR receptor,respectively 1. Troglitazone (2-200 M) is cytotoxic to the pancreatic cancer cell lines (MIA Paca2 andPANC-1 cells), with IC50s of 49.91.2 and 51.35.3 M, respectively. Troglitazone (50 M) increaseschromatin condensation in MIA Paca2 and PANC-1 cells, enhances the activit

6、y of caspase-3 and decreasesBcl-2 expression 2. Troglitazone (0, 1, 2, and 4 M) sensitizes TRAIL-mediated apoptosis in human lungadenocarcinoma cells. Troglitazone enhancement of TRAIL-induced apoptosis is blocked by inhibition ofautophagy, via activation of autophagy flux. In addition, the effects

7、of troglitazone are induced by PPARactivation in A549 cells 3.体内研究 Troglitazone (200 mg/kg, p.o.) shows inhibitory effects on the growth of tumor in the MIA Paca2 xenograftmodel 2.PROTOCOLCell Assay 2 Briefly, cells are seeded into 96-well plates at a density of 1105 cells/well and incubated for 24

8、h. The cellsare treated with Troglitazone in the presence or absence of other chemicals for a further 24 h using FBS-freemedium. The assay utilizes the conversion of alamar blue reagent to fluorescent resorufin by metabolicallyactive cells. The resorufin signal is measured at an excitation wavelengt

9、h of 530 nm and an emissionwavelength of 580 nm. The 50% growth inhibitory concentrations (IC50) are calculated according to thesigmoid inhibitory effect model E=IC50 /(IC50 +C), where E represents the surviving fraction (% ofcontrol), C represents the drug concentration in the medium, and represent

10、s the Hill coefficient. For co-exposure studies, the Troglitazone dosage is set to approximately the IC50 value for each cell line 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Balb/c male mice (4 weeks old) are subcutaneously inoculated in t

11、he back with MIA Paca2 cells (5106Administration 2 cells/100 L in PBS) 14 days prior to starting Troglitazone administration. Mice are then orally administered200 mg/kg Troglitazone in 0.5% methylcellulose solution or vehicle daily for 5 weeks. Tumor size ismeasured bi-dimensionally and the volume i

12、s calculated using the formula (lengthwidth2)0.5. Bodyweights of mice are also monitored throughout the experiment 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE Proc Natl Acad Sci U S A. 2

13、019 Feb 19;116(8):2996-3005. Toxicol Lett. 2018 Oct 1;295:379-389. Breast Cancer Res Treat. 2017 Oct;165(3):517-527. Drug Metab Dispos. 2019 Mar 28. Toxicol Mech Methods. 2019 Jul 25:1-24.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Willson TM, et al. The PPARs: from orphan

14、receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50.2. Fujita M, et al. In vitro and in vivo cytotoxicity of troglitazone in pancreatic cancer. J Exp Clin Cancer Res. 2017 Jul 3;36(1):91.3. Nazim UM, et al. PPAR activation by troglitazone enhances human lung cancer cells to TRAIL-induced apoptosis via autophagy flux.Oncotarget. 2017 Apr 18;8(16):