188048-45-5
| 中文名称 | 188048-45-5 |
|---|---|
| 中文同义词 | (±)-WS75624B;化合物 T13471 |
| 英文名称 | WS 75624 B |
| 英文同义词 | WS 75624 B;2-Pyridinecarboxylic acid, 6-[2-(6-hydroxyheptyl)-4-thiazolyl]-4,5-dimethoxy-;(±)-WS-75624B,(±)WS75624B,(±) WS75624B |
| CAS号 | 188048-45-5 |
| 分子式 | C18H24N2O5S |
| 分子量 | 380.46 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 188048-45-5.mol |
| 结构式 |  |
188048-45-5 性质
| 沸点 | 538.5±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.249±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 酸度系数(pKa) | 3.47±0.10(Predicted) |
IC50: 0.03 μg/mL (ECE)
Endothelin converting enzyme (ECE) inhibitors, WS75624A and (±)-WS75624B, have been isolated from the fermentation broth of Saccharothrix sp. No. 75624. WS75624A and (±)-WS75624B show highly potent ECE inhibitory activity, and both have IC 50 s of 0.03 μg/mL. WS75624A and (±)-WS75624B also show other metalloprotease (collagenase and neutral endopeptidase) inhibitory activity with IC 50 s of 1 μg/mL. (±)-WS75624B markedly inhibits ECE activity with an IC 50 value of 0.03 μg/mL, while it weakly inhibit collagenase and NEP activities with IC 50 s of 1.0 μg/mL and 1.25 μg/mL, respectively.
(±)-WS75624B inhibits big endothelin-induced pressor effect when administered to SD rat intravenously with big ET-1. WS75624 B (30 mg/kg) markedly attenuates the hypertensive effect of big ET-1 (1 nmol/kg,iv) the inhibiting the conversion of big ET-1 to ET-1.