Manidipine dihydrochloride 是一种钙离子通道阻断剂,能抑制钙流,IC50=2.6 nM。
产品描述
Manidipine dihydrochloride is a potent calcium channel blocker for Ca2+ current(IC50=2.6 nM).
体外活性
在高血压大鼠中,口服 Manidipine(3 mg/kg和10 mg/kg)以剂量依赖性的方式降低大鼠的收缩压.Manidipine(10 mg/kg)给药1小时到3小时后,能够将血压降低到正常水平.
体内活性
在纳摩尔级浓度的Manidipine,能够有效调节参与系膜细胞促炎性变化的基因转录。Manidipine抑制冠状动脉(pIC50=9.3 nM)和肾动脉(pIC50=9.1 nM)。Manidipine在高于0.1 nM浓度时降低Ca2+流,在100 nM浓度时阻断Ca2+流。
细胞实验
The mitogenic effect is measured by the amout of [3H]thymidine incorporated into DNA of human MCs and by assessment of cell proliferation. In brief, 1 × 105 quiescent cells is seeded into a 25-mL cell culture bottle and kept in low serum medium (0.1% FCS). On the following 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. The medium is replaced each day, and the cells are counted at days 1, 3 and 5.(Only for Reference)
Cas No.
89226-75-5
分子式
C35H40Cl2N4O6
分子量
683.63
别名
CV-4093;盐酸马尼地平;Manidipine 2HCl;Manidipine dihydrochloride
储存和溶解度
Ethanol:<1 mgml
H2O:<1 mgml
DMSO:20 mg/mL (29.3 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years