188048-45-5
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) |
188048-45-5 用途与合成方法
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.
