產(chǎn)品目錄

規(guī)格	1mg 5mg 10mg
CAS	130493-03-7
別名	N/A
化學(xué)名	N/A
分子式	C14H20ClN3O2
分子量	297.78
溶解度	Soluble in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

Bimoclomol is a heat shock protein (HSP) coinducer, used for treatment of cardiovascular diseases.

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 EC50 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[1]. 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[2]. 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[3].

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

[1]. Jednakovits A, et al. In vivo and in vitro acute cardiovascular effects of bimoclomol. Gen Pharmacol. 2000 May;34(5):363-9. [2]. Hargitai J, et al. Bimoclomol, a heat shock protein co-inducer, acts by the prolonged activation of heat shock factor-1. Biochem Biophys Res Commun. 2003 Aug 1;307(3):689-95. [3]. Polakowski JS, et al. Bimoclomol elevates heat shock protein 70 and cytoprotects rat neonatal cardiomyocytes. Eur J Pharmacol. 2002 Jan 18;435(1):73-7.

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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