INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC 50 s of 30 and 630 nM, respectively.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male 8-week old C57BKS/J db/db mice, control nondiabetic db/m miceDosage: 10, 20 mg/kg Administration: Intraperitoneal injection; daily for 2 weeks Result: Decreased plasma total cholesterol and triglyceride levels.