Nilvadipine是一种有效的钙离子通道抑制剂,IC50为0.03 nM。
别名:ARC029, FR34235
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).
分子量 | 385.37 |
分子式 | C19H19N3O6 |
CAS号 | 75530-68-6 |
溶解性(25°C) | DMSO 70 mg/mL |
储存条件 |
粉末型式 -20°C 3年;4°C 2年 溶于溶剂 -80°C 6个月;-20°C 1个月 |
运输方式 | 冰袋运输,根据产品的不同,可能会有相应调整。 |
*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前,需考虑其在不同溶剂中的溶解度限制。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.5949 mL | 12.9745 mL | 25.9491 mL |
5 mM | 0.519 mL | 2.5949 mL | 5.1898 mL |
10 mM | 0.2595 mL | 1.2975 mL | 2.5949 mL |
小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 | |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km 系数 | 3 | 6 | 12 | 8 | 5 | 20 |
动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
动物 A的Km系数 |
例如,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
[3] J Rosenthal. Nilvadipine: profile of a new calcium antagonist. An overview
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