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- Isradipine 75695-93-1

- Isradipine 75695-93-1
Isradipine 75695-93-1
产品描述 描述 Isradipine is a dihydropyridine calcium channel blockers with antihypertensive and vasodilator activities. Isradipine blocks the calcium entry through the calcium ion channels of coronary and peripheral vascular smooth muscle, thereby dilating coronary arteries and peripheral arterioles. This increases oxygen delivery due to an increased blood flow and reduces oxygen requirements due to decreasing in total peripheral resistance.
纯度 >98%储存/保存方法 Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.基本信息 别名 伊拉地平外观 黄色固体可溶性/溶解性 DMSO : 18.6 mg/mL (50 mM)
Ethanol : 7.4 mg/mL (20 mM)生物活性 靶点 Calcium channelIn vitro(体外研究) Isradipine produces inhibition of both growth cultures and oxygen consumption on epimastigotes of Trypanosoma cruzi Tulahuen strain, at micromolar concentrations. Isradipine is found to be the most potent derivative in both, in growth cultures (I50 = 20.8 mM) and in vivo oxygen uptake (I50 = 31.1 mM).In vivo(体内研究) Isradipine reduces hypoxia-induced activation of calcium dependent xanthine oxidases, monoamine oxidases, cytosolic phospholipase A(2) and cyclooxygenases (COX-2) along with concomitant decrease in free radical generation and cytochrome c release. Isradipine prevents hypobaric hypoxia along with augmented neurodegeneration and memory impairment induced increased expression of calpain and caspase 3. Isradipine (at the dose of 1 mg/kg three times a day) reduces ethanol intake by over 70% in ethanol-preferring rats, the reduction in ethanol intake is compensated by a proportional increase in water consumption and the inhibitory effect persisted throughout the 5 days of treatment. Isradipine significantly reduces the arterial wall collagen contents in both strains, with marked increases in the elastin content in the carotid but not in the aortic wall in spontaneously hypertensive rats. Isradipine suppresses the reinforcing properties of morphine and cocaine and may be an effective pharmacotherapy for treatment of cocaine and heron abuse in mice.参考文献 参考文献 1. Ilijic E, et al. Neurobiol Dis. 2011 Aug;43(2):364-71.
2. Anekonda TS, et al. Biochim Biophys Acta. 2011 Dec;1812(12):1584-90.
研究领域 研究领域 Drug DiscoverySmall Molecule DrugLead Compound DiscoveryIsradipine 75695-93-1温馨提示:本产品仅作科研实验使用,不支持临床等研究
