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130493-03-7

中文名稱 bimoclomol
英文名稱 bimoclomol
CAS 130493-03-7
分子式 C14H20ClN3O2
分子量 297.78
MOL 文件 130493-03-7.mol
130493-03-7 結構式 130493-03-7 結構式

基本信息

中文別名
氯吡哌醇
化合物 T13580
英文別名
bimoclomol
3-Pyridinecarboximidoyl chloride, N-[2-hydroxy-3-(1-piperidinyl)propoxy]-

物理化學性質

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)Oil
顏色Light yellow to brown

常見問題列表

生物活性
Bimoclomol 是一種 heat shock protein (HSP) 輔誘導劑,可用于心血管疾病的研究。
靶點

HSP

體外研究

Bimoclomol (40 μM) significantly increases coronary flow (CF) in the period of normoxic perfusion (before ischemia). Bimoclomol significantly increases LVDP and CO, but it decreases LVEDP under ischemic conditions. Bimoclomol displays a biphasic effect on the rate of relaxation. Bimoclomol (>10 μM) causes concentration-dependent vasorelaxation, with EC 50 value of 214 μM. Bimoclomol (100 μM) induces vasorelaxation also against 20 mM KCl. However, bimoclomol fails to relax preparations precontracted with serotonin, PGF2 or angiotensin II. Bimoclomol does not affect the stability of Hsp70 or its mRNA. Bimoclomol coinduces Hsp expression via the prolonged activation of the heat shock transcription factor (HSF-1). The effects of bimoclomol are abolished in cells from mice lacking HSF-1. Furthermore, bimoclomol can bind to HSF-1 and induce a prolonged binding of HSF-1 to the respective DNA elements. Bimoclomol (0.1, 1 and 10 μM) improves cell survival of rat neonatal cardiomyocytes compared to vehicle-treated cells. Bimoclomol (0.01 to 10 μM) significantly elevates HSP70 levels, based on the time of exposure. Pretreatment with bimoclomol for 24 h significantly increases survival of cells.

體內研究

Bimoclomol (1 and 5 mg/kg) decreases the ST-segment elevation induced by coronary occlusion by 56% and 80%, respectively, in anesthetized dogs.

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