生物活性

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).

化学数据

不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

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K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

储备液配制

以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。