SB756050 是选择性的 TGR5 激动剂。SB756050有潜力用于二型糖尿病的研究。

SB756050 is a selective TGR5 agonist. SB756050 has the potential for type 2 diabetes treatment.

Solid

TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D). has not independently confirmed the accuracy of these methods. They are for reference only.

SB756050 is well‐tolerated; it is readily absorbed, exhibited nonlinear pharmacokinetics with a less than dose‐proportional increase in plasma exposure above 100 mg, and demonstrates no significant changes in exposure when co‐administered with sitagliptin. SB756050 demonstrates highly variable pharmacodynamic effects both within dose groups and between doses, with increases in glucose seen at the two lowest doses and no reduction in glucose seen at the two highest doses. The glucose effects of SB756050 sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Hodge RJ, et al. Safety, Pharmacokinetics, and Pharmacodynamic Effects of a Selective TGR5 Agonist, SB-756050, in Type 2 Diabetes. Clin Pharmacol Drug Dev. 2013 Jul;2(3):213-22.

In Vitro: DMSO : ≥ 150 mg/mL (299.65 mM)配制储备液