447410-57-3
中文名称
447410-57-3
英文名称
SB-756050
CAS
447410-57-3
分子式
C21H28N2O8S2
分子量
500.59
MOL 文件
447410-57-3.mol
更新日期
2024/05/27 17:16:38
447410-57-3 结构式
基本信息
中文别名
化合物SB7560501,4-双((3,4-二甲氧基苯基)磺酰基)-1,4-二氮杂环庚烷
英文别名
SB-756050SB-756050, >98%
SB756050
SB 756050
SB-756050
1,4-bis((3,4-dimethoxyphenyl)sulfonyl)-1,4-diazepane
1H-1,4-Diazepine, 1,4-bis[(3,4-dimethoxyphenyl)sulfonyl]hexahydro-
物理化学性质
沸点653.1±65.0 °C(Predicted)
密度1.328±0.06 g/cm3(Predicted)
储存条件-20°C储存
溶解度DMF: 10 mg/ml; DMF:PBS (pH 7.2) (1:2): 0.25 mg/ml; DMSO: 10 mg/ml
酸度系数(pKa)-6.97±0.20(Predicted)
形态结晶固体
常见问题列表
生物活性
SB-756050是选择性TGR5激动剂，对人源TGR5的EC50值为1.3 μM。靶点
| Target | Value |
|
TGR5
() |
体外研究
TGR5 is a bile acid receptor and a potential target for the treatment of type 2 diabetes (T2D).
体内研究
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.