T0901317 - FXR Agonist - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemET0901317Cat. No.: HY-10626CAS No.: 293754-55-9分式: CHFNOS分量: 481.33作靶點: FXR; LXR作通路: Metabolic Enzyme/Protease儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 100 mg/mL (207.76 mM)Methanol :

2、100 mg/mL (207.76 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.0776 mL 10.3879 mL 20.7758 mL5 mM 0.4155 mL 2.0776 mL 4.1552 mL10 mM 0.2078 mL 1.0388 mL 2.0776 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次?/p>

3、加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，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. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (6.23 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3 mg/mL (6.23 mM); Clear solution1/3 Master of Small Mo

4、lecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 3 mg/mL (6.23 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 T0901317有效，選擇性的 LXR 和 FXR 激動劑，EC50 分別為 50 nM 和 5 M。T0901317 通過 LXR 依賴性機制誘導(dǎo)其抗增殖和細(xì)胞毒性作。T0901317 以劑量和時間依賴性式顯著抑制細(xì)胞增殖并誘導(dǎo)細(xì)胞程序性死亡。 T0901317 可以抑制脂 飲引起的肥胖，降低胰島素。IC50 & Target FXR,

5、 LXR 1,2體外研究T0901317 (5-50 M; 72 hours) significantly inhibits cellular proliferation in all cell lines in a dose-dependentand time-dependent manner 3.T0901317 (10 M; 24-72 hours) decreases the percentage of cells in S phase and increases the percentageof cells in the G0/G1 phase, indicating a cell

6、cycle arrest at the G1-S checkpoint. The percentage of cells inG0/G1 phase increases in a time-dependent manner 3.T0901317 (10-40 M; 24 hours ) results in a significant increase of cells in early apoptosis 3.T0901317 (5-40 M; 48 hours) results in an increase of p21 and p27 protein expression in a do

7、se-dependentmanner after 48 hours 3.Cell Proliferation Assay 3Cell Line: A2780, CaOV3 and SKOV3 ovarian cancer cell linesConcentration: 5, 10, 20, 40 or 50 MIncubation Time: 72 hoursResult: Inhibited cellular proliferation in all cell lines in a dose-dependent and time-dependentmanner.Cell Cycle Ana

8、lysis 3Cell Line: A2780, CaOV3 and SKOV3 cellsConcentration: 10 MIncubation Time: 24, 48 or 72 hoursResult: Decreased the percentage of cells in S phase and increased the percentage of cells inthe G0/G1 phase.Apoptosis Analysis 3Cell Line: CaOV3 cellsConcentration: 10 to 40 M2/3 Master of Small Mole

9、cules 您邊的抑制劑師www.MedChemEIncubation Time: 24 hoursResult: Resulted in a significant increase of cells in early apoptosis.Western Blot Analysis 3Cell Line: CaOV3 cellsConcentration: 5 to 40 MIncubation Time: 48 hoursResult: Resulted in an increase of p21 and p27 protein expression in a dose-dependent

10、 manner.體內(nèi)研究 T0901317 (i.p.; 50 mg/kg; twice weekly for 7 days) significantly slowes down the weight gain of C57/BL6mice 4 .Animal Model: Male C57BL/6 mice 4Dosage: 50 mg/kgAdministration: I.p.; twice weekly; for 7 daysResult: Slowed down the weight gain of C57/BL6 mice.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Anal Chem. 2019 J

11、an 15;91(2):1501-1506.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Ding H et al. LXR agonist T0901317 upregulates thrombomodulin expression in glomerular endothelial cells by inhibition of nuclearfactor?B. Mol Med Rep. 2016 Jun;13(6):4888-962. Baranowski M et al. Insulin-sen

12、sitizing effect of LXR agonist T0901317 in high-fat fed rats is associated with restored muscle GLUT4expression and insulin-stimulated AS160 phosphorylation. Cell Physiol Biochem. 2014;33(4):1047-53. Rough JJ, et al. Anti-proliferative effect of LXR agonist T0901317 in ovarian carcinoma cells. J Ovarian Res. 2010 May 26;3:13.4. Gao M, et al. The liver X receptor agonist T0901317 protects mice from high fat diet-induced obesity and insulin resistance. AAPS J.2013 Jan;15(1):258-66.McePdfHeightC