188048-45-5 (±)-WS75624B

• 生物活性 (±)-WS75624B 是一种内皮素转化酶 (ECE) 抑制剂，IC50 为 0.03 μg/mL。
• 靶点 IC50: 0.03 μg/mL (ECE)
• 体外研究 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.
• 体内研究 (±)-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.

医药

提取方法

• 来源: 从Saccharothrix sp. No. 75624的发酵液中分离得到WS75624A和(±)-WS75624B。
• 活性验证: 两者均显示强效ECE抑制活性，IC50为0.03 μg/mL；同时对胶原酶和中性内肽酶也有抑制作用，IC50分别为1 μg/mL和1.25 μg/mL。