447410-57-3
| 中文名称 | 447410-57-3 |
|---|---|
| 中文同义词 | 化合物SB756050;1,4-双((3,4-二甲氧基苯基)磺酰基)-1,4-二氮杂环庚烷 |
| 英文名称 | SB-756050 |
| 英文同义词 | SB-756050;1,4-bis((3,4-dimethoxyphenyl)sulfonyl)-1,4-diazepane;SB756050;SB 756050;SB-756050;SB-756050, >98%;1H-1,4-Diazepine, 1,4-bis[(3,4-dimethoxyphenyl)sulfonyl]hexahydro-;G protein-coupled Bile Acid Receptor 1,inhibit,TGR5,Inhibitor,SB756050,GPBAR1,G-protein coupled receptor 19,GPCR19 |
| CAS号 | 447410-57-3 |
| 分子式 | C21H28N2O8S2 |
| 分子量 | 500.59 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 447410-57-3.mol |
| 结构式 |  |
447410-57-3 性质
| 沸点 | 653.1±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.328±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMF：10mg/mL； DMF:PBS (pH 7.2) (1:2)：0.25 mg/mL；二甲基亚砜：10mg/mL |
| 形态 | 结晶固体 |
| 酸度系数(pKa) | -6.97±0.20(Predicted) |
SB-756050是选择性TGR5激动剂，对人源TGR5的EC50值为1.3 μM。
| Target | Value |
|
TGR5
() |
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-102016 | SB756050 | 5 mg | 350元 | |
| 2024/04/30 | HY-102016 | 447410-57-3 SB756050 | 447410-57-3 | 10mM * 1mLin DMSO | 385元 |