Manidipine 2HCl是Manidipine的盐酸盐形式,是钙通道(Calcium Channel)阻断剂,IC50为2.6 nM。
别名:CV-4093
Manidipine dihydrochloride (CV-4093) is a hydrochloride salt of manidipine that is a lipophilic, third-generation, highly vasoselective dihydropyridine calcium antagonist with an IC50 of 2.6 nM. Manidipine dihydrochloride (CV-4093) causes systemic vasodilation by inhibiting the voltage-dependent calcium inward currents in smooth muscle cells. Manidipine dihydrochloride (CV-4093) is used clinically as an antihypertensive. Manidipine dihydrochloride (CV-4093) suppressed the DNA synthesis of vascular smooth muscle cells (VSMC) dose dependently at concentrations of more than 10 nM. Mandipine hydrochloride (1 uM) suppressed proliferation of VSMC to 50% of the control value. Manidipine hydrochloride stimulated the synthesis of GAG at concentrations above 0.01 nM. Manidipine hydrochloride (10 nM) stimulated synthesis of glycosaminoglycans (GAG) to 450% of control.
体外实验* | |
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细胞系 | Mesangial cells |
方法 | Measuring the mitogenic effect by the amout of [3H]thymidine incorporated into DNA of human MCs and by assessment of cell proliferation. In brief, seeding 1 ?105 quiescent cells into a 25-mL cell culture bottle and keeping in low serum medium (0.1% FCS). On the next day, the cells are preincubated for 3 hours with Manidipine (10 nM) followed by stimulation with PDGF-BB (10 ng/mL) or incubated with low serum medium abone. Replacing the medium each day, and counting the cells at days 1, 3 and 5. |
浓度 | 10 nM |
处理时间 | Days 1, 3 and 5 |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
体内实验* | |
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动物模型 | Normotensive male Wistar-Kyoto rats and male stroke-prone SHR |
配制 | Saline |
剂量 | 1 mg/kg, 3 mg/kg and 10 mg/kg |
给药处理 | Administered via p.o. |
*上述方法来自公开文献,仅供相同目的实验参考。如实验目的、材料、方法不同,请参考其他文献。
分子量 | 683.62 |
分子式 | C35H38N4O6.2HCl |
CAS号 | 89226-75-5 |
溶解性(25°C) | DMSO 20 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 | 1.4628 mL | 7.314 mL | 14.628 mL |
5 mM | 0.2926 mL | 1.4628 mL | 2.9256 mL |
10 mM | 0.1463 mL | 0.7314 mL | 1.4628 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。
[1] Luca Cavalieri, et al. Metabolic effects of manidipine
[2] Paul L McCormack, et al. Delapril/manidipine
[3] Alex Roca-Cusachs, et al. Antihypertensive effect of manidipine
[4] Kate McKeage, et al. Manidipine: a review of its use in the management of hypertension
[5] S M Cheer, et al. Manidipine: a review of its use in hypertension
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