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- Lacidipine 103890-78-4

- Lacidipine 103890-78-4
Lacidipine 103890-78-4
产品描述 描述 Lacidipine (Lacipil, Motens) is a L-type calcium channel blocker.Lacidipine, a novel third-generation dihydropyridine calcium channel blocker, has been demonstrated effective for hypertension. lacidipine protects HKCs against apoptosis induced by ATP depl
纯度 99%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 拉西di平外观 白色至灰白色结晶固体可溶性/溶解性 DMSO : 84 mg/mL (184.4 mM)
Ethanol : 21 mg/mL (46.1 mM)生物活性 靶点 L-type calcium channelIn vitro(体外研究) Lacidipine, an L-type Ca(2+) channel blocker that also inhibits (ER) efflux, enhances folding, trafficking, and activity of degradation-prone glucocerebrosidase (GC) variants. Lacidipine remodels mutated GC proteostasis by simultaneously activating a series of distinct molecular mechanisms, namely modulation of Ca(2+) homeostasis, upregulation of the ER chaperone BiP, and moderate induction of the unfolded protein response. Lacidipine almost completely inhibits cholesterol esterification in cholesterol loaded mouse cultured peritoneal macrophages.In vivo(体内研究) Lacidipine has non-significant effects on blood pressure but inhibits the paradoxical increases in plasma renin activity (PRA) and in renin mRNA in kidney that are found in salt-loaded stroke-prone spontaneously hypertensive rats (SHRSP). Lacidipine restores the physiological downregulation of renin production by high salt and reduces left ventricular hypertrophy and mRNA levels of atrial natriuretic factor and transforming growth factor-beta1. Lacidipine (1 and 3 mg/kg) also effectively increases calcium concentrations significantly in ovariectomized rats. Lacidipine, a dihydropyridine-type calcium antagonist, reduces the cardiac hypertrophy and the cardiacendothelin-1 (ET-1) gene overexpression occurring in salt-loaded stroke-prone spontaneously hypertensive rats (SL-SHRSP), an effect occurring without systolic blood pressure (SBP) change. Lacidipine exerts a dose-related inhibition of ventricle hypertrophy and preproET-1-mRNA expression in SHRSP and indicate that this effect is unrelated to SBP changes.参考文献 参考文献 1. Huai Y, et al. Eur J Pharmacol. 2013 Oct 15;718(1-3):441-7.
2. Liu X, et al. Int J Cardiol. 2013 Oct 9;168(4):3317-26.
研究领域 研究领域 CardiovascularDrug DiscoverySmall Molecule DrugLead Compound DiscoveryLacidipine 103890-78-4温馨提示:本产品仅作科研实验使用,不支持临床等研究
