4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
产品详情
INT-767 是法尼醇 X 受体 (FXR)/TGR5双激动剂,EC50 值分别为 30 和 630 nM。
生物活性
INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC 50 s of 30 and 630 nM, respectively.
性状
Solid
体外研究(In Vitro)
INT-767 does not show cytotoxic effects in HepG2 cells, does not inhibit cytochrome P450 enzymes, is highly stable to phase I and II enzymatic modifications, and does not inhibit the human ether-a-go-go -related gene potassium channel. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
INT-767 (10-20 mg/kg; i.p.; daily for 2 weeks) decreases plasma total cholesterol and triglyceride levels in db/m and db/db mice . has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Male
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Baghdasaryan A, et al. Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the 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 andTGR5 agonist. Mol Pharmacol. 2010 Oct;78(4):617-630.
溶解度数据
In Vitro: DMSO : ≥ 100 mg/mL (202.16 mM)H2O : 100 mg/mL (202.16 mM; Need ultrasonic)