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188048-45-5

中文名稱 188048-45-5
英文名稱 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 結(jié)構(gòu)式 188048-45-5 結(jié)構(gòu)式

基本信息

中文別名
(&PLUSMN
)-WS75624B
英文別名
WS 75624 B
2-Pyridinecarboxylic acid, 6-[2-(6-hydroxyheptyl)-4-thiazolyl]-4,5-dimethoxy-

物理化學(xué)性質(zhì)

沸點538.5±50.0 °C(Predicted)
密度1.249±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)3.47±0.10(Predicted)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335

常見問題列表

生物活性
(±)-WS75624B 是一種內(nèi)皮素轉(zhuǎn)化酶 (ECE) 抑制劑,IC50 為 0.03 μg/mL。
靶點

IC50: 0.03 μg/mL (ECE)

體外研究

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.

體內(nèi)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.

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