生物活性
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.
化学数据
| 分子量 | 683.62 |
| 分子式 | C35H38N4O6.2HCl |
| CAS号 | 89226-75-5 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO 20 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 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 |
| 动物实验 |
|---|
| 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. |
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）
| 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。
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。
| 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 |
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