Manidipine 2HCl (CV-4093) 是一种二氢吡啶化合物和钙通道阻滞剂,作用于 Ca2+ 电流,IC50 为 2.6 nM。
Cas No. | 89226-75-5 |
别名 | 盐酸马尼地平,CV-4093 |
化学名 | 5-O-[2-(4-benzhydrylpiperazin-1-yl)ethyl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate;dihydrochloride |
Canonical SMILES | CC1=C(C(C(=C(N1)C)C(=O)OCCN2CCN(CC2)C(C3=CC=CC=C3)C4=CC=CC=C4)C5=CC(=CC=C5)[N+](=O)[O-])C(=O)OC.Cl.Cl |
分子式 | C35H40Cl2N4O6 |
分子量 | 683.62 |
溶解度 | ≥ 69mg/mL in DMSO with gentle warming, ≥ 69.2mg/mL in EtOH with gentle warming |
储存条件 | 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 |
产品描述 | Manidipine dihydrochloride (CV-4093) is a dihydropyridine compound and a calcium channel blocker for Ca2+ current with IC50 of 2.6 nM. IC50 value: 2.6 nMTarget: calcium channelManidipine dihydrochloride is described to block T-type Ca2+ channels specifically and is also described to have a high selectivity for the vasculature, presenting negligible cardiodepression as compared to other Ca2+ channel antagonists. Manidipine is also described to not significantly affect norepinephrine levels, suggesting a lack of sympathetic activation with this compound. Manidipine reduces pro-inflammatory cytokines secretion in human endothelial cells and macrophages. Manidipine, unlike other third-generation dihydropyridine derived drugs, blocks T-type calcium channels present in the efferent glomerular arterioles, reducing intraglomerular pressure and microalbuminuria. References: [1]. Buset Ríos N, Rodríguez Esparragón F, Fernández-Andrade Rodríguez C, et al. Vascular and metabolic properties of manidipine . Nefrologia. 2011;31(3):268-74. [2]. Costa S, Zimetti F, Pedrelli M, et al. Manidipine reduces pro-inflammatory cytokines secretion in human endothelial cells and macrophages. Pharmacol Res. 2010 Sep;62(3):265-70. [3]. Cavalieri L, Cremonesi G. Metabolic effects of manidipine. Am J Cardiovasc Drugs. 2009;9(3):163-76. doi: 10.2165/00129784-200909030-00004. [4]. Roca-Cusachs A, Triposkiadis F. Antihypertensive effect of manidipine. Drugs. 2005;65 Suppl 2:11-9. [5]. Nagaoka A. Pharmacologic characteristics of a new calcium antagonist, manidipine: beneficial effects on renal circulation and vascular changes. Am Heart J. 1993 Feb;125(2 Pt 2):560-5. |