Nilvadipine,75530-68-6

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产品名称：Nilvadipine

产品别名：尼伐地平

英文别名：FK235;FR34235

靶点：Calcium channel

CAS：75530-68-6

纯度：>98%

外观：黄色结晶性粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Nilvadipine (ARC029) is a potent calcium channel blocker with an IC50 of 0.03 nM. Nilvadipine (ARC029) is used for the treatment of hypertension and chronic major cerebral artery occlusion. Nilvadipine (ARC029) were administrated? intramuscularly in daily doses of 0.01-10 mg/kg for three weeks, starting on the day of cuff-placement. Nilvadipine (ARC029) prvented the cuff-induced intimal thickening in a dose-dependent manner, and was more potent than the other calcium antagonists including nifedipine, diltiazem and verapamil. In an in vitro experiment on inhibition of migration of rat aortic smooth muscle cells, using zymosan-activated air pouch exudate as a chemoattractant in modified Boyden chambers, Nilvadipine (ARC029) was also the most potent among the calcium antagonists tested. The IC50 values were 0.17 nM for nifedipine, 6 nM for verapamil and 0.24 mM for diltiazem. Effects of these drugs on proliferation of rat aortic smooth muscle cells and rabbit platelet aggregation were also examined in vitro. At concentrations less than 10 mM, none of the drugs inhibited proliferation of the smooth muscle cells, and only verapamil inhibited collagen-induced platelet aggregation (IC50 = 0.9 mM).

溶解性：Ethanol ：19.3 mg/mL (50 mM)
DMSO ：38.5 mg/mL (100 mM)

体外研究：

Nilvadipine strongly inhibits the chemotaxis of interleukin-1 (IL-1), leukotriene B4 (LTB4), platelet-derived growth factor (PDGF) with IC50 of 0.1 nM in rat aortic smooth muscle cells (SMC). Nilvadipine is reported to increase renal blood flow and reduce filtration fraction in the isolated perfused hydronephrotic kidney, suggesting indirectly afferent and efferent arteriolar vasodilation.

体内研究：Nilvadipine preserves retinal morphology and electroretinogram responses in RCS rats during the initial stage of retinal degeneration. Nilvadipine significantly enhances rhodopsin kinase and alphaA-crystallin expression and suppression of caspase 1 and 2 expression in the retina of RCS rats. Nilvadipine completely inhibits the vasoactivity elicited by Abeta in rat aortae and in human middle cerebral arteries. Nilvadipine restores cortical perfusion levels in Tg APPsw to values similar to those observed in control littermates without notably affecting the CBF of control mice. Nilvadipine suppresses ischemia (20 min)-reflow (20 min)-induced paw edema of mice (ED30:0.4 mg/kg i.v. and 2 mg/kg p.o.). Nilvadipine suppresses carrageenan-induced paw edema (ED30:15 mg/kg in rats and 20 mg/kg in mice) at a potency corresponding to that of an anti-inflammatory drug, ibuprofen. Nifedipine, nicardipine and nimodipine results in a suppression of 30% only with 100 mg/kg oral dosing in rats. Nilvadipine inhibits superoxide radical (O-2production from xanthine oxidase (XOD) both with lactate dehydrogenase + NADH method and cytochrome c method (IC50:90 and 100 mg/mL, respectively).

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