INT-767-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEINT-767Cat. No.: HY-12434CAS No.: 1000403-03-1分式: CHNaOS分量: 494.66作靶点: FXR; GPCR19作通路: Metabolic Enzyme/Protease; GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 205.5 mg/mL (

2、415.44 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.0216 mL 10.1080 mL 20.2159 mL5 mM 0.4043 mL 2.0216 mL 4.0432 mL10 mM 0.2022 mL 1.0108 mL 2.0216 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。BIOLOGICAL ACTIVITY物活性 INT-767是法尼醇 X 受体 (FXR)/TGR5双激动剂，

3、EC50 值分别为 30 和 630 nM 1 2。体外研究 INT-767 does not show cytotoxic effects in HepG2 cells, does not inhibit cytochrome P450 enzymes, is highlystable to phase I and II enzymatic modifications, and does not inhibit the human ether-a-go-go-related genepotassium channel 2.1/2 Master of Small Molecules 您边的抑制

4、剂师www.MedChemE体内研究 INT-767 (10-20 mg/kg; i.p.; daily for 2 weeks) decreases plasma total cholesterol and triglyceride levels indb/m and db/db mice 2.Animal Model: Male 8-week old C57BKS/J db/db mice, control nondiabetic db/m mice 2Dosage: 10, 20 mg/kgAdministration: Intraperitoneal injection; daily

5、for 2 weeksResult: Decreased plasma total cholesterol and triglyceride levels.户使本产品发表的科研献 J Am Soc Nephrol. 2018 Nov;29(11):2658-2670.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Baghdasaryan A, et al. Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in th

6、e Mdr2-/- (Abcb4-/-)mousecholangiopathy model by promoting biliary HCO3- output. Hepatology. 2011 Oct;54(4):1303-1312.2. Rizzo G, et al. Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor andTGR5agonist. Mol Pharmacol. 2010 Oct;78(4):617-630.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 40