Lemildipine ≥98%
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| 包装规格: | 5mg in glass bottle |
| 溶解性: | 溶于DMSO(100mg/ml超声) |
| 产品描述: | 基本信息 产品编号: L10495 产品名称: Lemildipine CAS: 94739-29-4 储存条件 粉末 -20℃ 四年 分子式: C20H22Cl2N2O6 溶于液体 -80℃ 6个月 分子量: 457.30 -20℃ 1个月 化学名: 5-O-methyl 3-O-propan-2-yl 2-(carbamoyloxymethyl)-4-(2,3-dichlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate Solubility (25°C): 体外: DMSO Ethanol Water 体内(现配现用): <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 制备储备液 浓度 溶液体积 质量 1mg 5mg 10mg 1mM 2.1867mL 10.9337mL 21.8675mL 5mM 0.4373mL 2.1867mL 4.3735mL 10mM 0.2187mL 1.0934mL 2.1867mL 生物活性 产品描述 一种钙通道阻滞剂。 靶点 Calcium entry 体内研究 Gerbils are treated intraperitoneally with Lemildipine (0.1-3mg/kg) just after release of the occlusion.Four days after the ischemia,they are fixed by perfusing 10% buffered-formalin,and the neuronal cell density (NCD,cell/mm) in the CA1 subfield is estimated under microscopy.The average NCD in the ischemic control group is 43±10.8 cells/mm,whereas Lemildipine (3mg/kg) significantly ameliorates DND with an average NCD of 143±24.2 cells/mm (P<0.01).In addition,Lemildipine (3mg/kg) significantly inhibits delayed neuronal death (DND) at 1,2 and 4 weeks after transient ischemia:the average NCD of the Lemildipine and ischemic control groups are 80±9.4 (P<0.01) and 43±7.7 cells/mm,92±13.7 (P<0.05) and 52±9.3 cells/mm,and 57±5.0 (P<0.01) and 43±12.4 cells/mm,respectively.In this experiment,Lemildipine (NB-818) exhibits a protective effect on DND in the hippocampal CA1 subfield after transient forebrain ischemia, and its effect persisted for up to 4 weeks.In normal Wistar rats (NWR),Lemildipine (NPK-1886) in doses of 3-30mg/kg,p.o.,produces a mild lowering of blood pressure.The depressor effect of Lemildipine is much the same as that of Nifedipine. In contrast,Lemildipine produces a significant decrease in the blood pressure of spontaneously hypertensive rats (SHR).Oral administration of Lemildipine in doses of 3,10,30mg/kg produces a significant decrease in systolic blood pressure dose-dependently.The maximum decrease is observed 1-3hr after administration.Comparing the hypotensive potency of Lemildipine and Nifedipine,their dose-response curves at the maximum response during the observation (for 24hr) are analyzed by the least squares method,and the dose of 30% decrease in blood pressure from the control level (ED30) are used as a measure of their potency.Lemildipine is 1.4 times stronger than Nifedipine;the ED30 values of Lemildipine and Nifedipine are 10.2mg/kg and 14.3mg/kg,respectively. 推荐实验方法(仅供参考) 动物实验: Gerbils Male Mongolian gerbils,weighing 50-80g,are used in this experiment.Lemildipine (3mg/kg) or vehicle is administered intraperitoneally just after the recirculation. At 1,2 or 4 weeks after ischemia,the animals are sacrificed,and the protective effect of Lemildipine (NB-818) is examined. Mice and Rats Normal Wistar rats (NWR) and hypertensive model rats (spontaneously hypertensive rats (SHR),renal hypertensive rats (RHR) and DOCA-saline-induced hypertensive rats (DOC-Na-R)) of the male sex, weighing from 250 to 350g,are used.Oral administration of Lemildipine in doses of 3,10,30mg/kg for normal Wistar rats (NWR).Lethal dose of Lemildipine and Nifedipine is determined by the Litchfield-Wilcoxon method from the data of experiments using healthy mice and rats.Mice (male and female) weighing 20±2g and male rats weighing from 150 to 220g are used.These two kinds of animals are fed on solid food (Crea,CA-1) and water ad lib.The animal room temperature and humidity are controlled at 22±2℃ and 55±5%,respecttively.No food except water is administered 24hr before starting the experiments for oral administration of drugs. |
| 保存条件: | -20℃ |
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