SB756050 是TGR5选择性激动剂。它用于二型糖尿病研究的潜力。

SB756050 is a specific TGR5 agonist.

TGR5 is a potential target for the therapy of type 2 diabetes (T2D). Thus, SB756050 is used in phase 1clinical trials for the treatment of type 2 diabetes.

SB756050 is well‐ olerated with nonlinear pharmacokinetics. It shows dose‐proportional increase in plasma exposure above 100 mg, and has no marked changes in exposure when co‐administered with sitagliptin. SB756050 has highly variable pharmacodynamic effects both within between doses and dose groups, 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 t sitagliptin are comparable to those of sitagliptin alone, even though gut hormone plasma profiles are different.

447410-57-3

C21H28N2O8S2

500.58

SB 756050;SB-756050

DMSO:150 mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years