SB-756050

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB756050 是一种特定的 TGR5 激动剂。

SB-756050 is a G protein-coupled bile acid receptor 1 (GPBAR1) agonist potentially for the treatment of type 2 diabetes.(In Vivo):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.

TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D).

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.

SB-756050 | SB 756050 | SB756050

Cell Cycle/DNA Damage

DNA/RNA Synthesis

TGR5

——

——

447410-57-3

500.59

C21H28N2O8S2

>98% (HPLC)

DMSO : ≥ 150 mg/mL; 299.65 mM

O=S(=O)(N1CCN(S(=O)(=O)c2ccc(OC)c(OC)c2)CCC1)c1ccc(OC)c(OC)c1

1,4-bis((3,4-dimethoxyphenyl)sulfonyl)-1,4-diazepane

(-20℃)

With Ice Pack

≥ 2 years