188048-45-5

中文名称 188048-45-5

英文名称 WS 75624 B

CAS 188048-45-5

分子式 C18H24N2O5S

分子量 380.46

MOL 文件 188048-45-5.mol

188048-45-5 结构式

基本信息物理化学性质安全数据常见问题列表

基本信息

中文别名

(&PLUSMN
)-WS75624B

英文别名

WS 75624 B
2-Pyridinecarboxylic acid, 6-[2-(6-hydroxyheptyl)-4-thiazolyl]-4,5-dimethoxy-

物理化学性质

沸点538.5±50.0 °C(Predicted)

密度1.249±0.06 g/cm3(Predicted)

储存条件-20°C储存

溶解度溶于二甲基亚砜

酸度系数(pKa)3.47±0.10(Predicted)

安全数据

危险性符号(GHS) GHS hazard pictograms

GHS07

警示词警告

危险性描述H302-H315-H319-H335

防范说明P261-P305+P351+P338

常见问题列表

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.