Troglitazone-CS-045-DataSheet-生命科學(xué)試劑-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作靶點(diǎn): PPAR; Autophagy作通路: Cell Cycle/DNA Damage; Autophagy儲(chǔ)存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL

2、(226.48 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)

3、結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.66 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.66 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% c

4、orn oil1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (5.66 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 TroglitazonePPAR 的激動(dòng)劑，對(duì)和 PPAR的 EC50 值分別為 550 nM 和 780 nM。IC50 & Target PPAR550 nM (EC50, Human PPAR)體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn)2/3 Master of Small Molecules 您邊的抑制劑師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):