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Nitrendipine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nitrendipine图片
CAS NO:39562-70-4
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议

产品介绍
Nitrendipine (BAY-E-5009) 是 Nifedipine 的类似物,是一种具有血管扩张作用的二氢吡啶类钙通道阻滞剂。
Cas No.39562-70-4
别名尼群地平; BAY-E-5009
化学名5-O-ethyl 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
Canonical SMILESCCOC(=O)C1=C(NC(=C(C1C2=CC(=CC=C2)[N+](=O)[O-])C(=O)OC)C)C
分子式C18H20N2O6
分子量360.3699
溶解度≥ 13.7mg/mL in DMSO
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Nitrendipine is a calcium channel blocker with marked vasodilator action.Target: Calcium ChannelNitrendipine is a dihydropyridine calcium channel blocker. It is used in the treatment of primary hypertension to decrease blood pressure. Nitrendipine blocked Ca2+ currents very potently, with half-block by subnanomolar concentrations. The concentration dependence of block had the form expected for 1:1 binding, with an apparent dissociation constant (Kd) of 0.36 nM. In contrast, when cells were held at hyperpolarized potentials, nitrendipine blocked Ca2+ currents much less potently (Kd approximately equal to 700 nM) [1, 2]. Nitrendipine, a potent analogue of nifedipine, binds in a reversible and saturable manner to partially purified guinea-pig heart membranes [3]. [3H]nitrendipine binding in smooth muscle is to a site which mediates the pharmacologic response [4].

References:
[1]. Bean, B.P., Nitrendipine block of cardiac calcium channels: high-affinity binding to the inactivated state. Proc Natl Acad Sci U S A, 1984. 81(20): p. 6388-92.
[2]. Peterson, B.Z., T.N. Tanada, and W.A. Catterall, Molecular determinants of high affinity dihydropyridine binding in L-type calcium channels. J Biol Chem, 1996. 271(10): p. 5293-6.
[3]. Bellemann, P., et al., [3H]-Nitrendipine, a potent calcium antagonist, binds with high affinity to cardiac membranes. Arzneimittelforschung, 1981. 31(12): p. 2064-7.
[4]. Bolger, G.T., et al., Characterization of binding of the Ca++ channel antagonist, [3H]nitrendipine, to guinea-pig ileal smooth muscle. J Pharmacol Exp Ther, 1983. 225(2): p. 291-309.