产品
编 号：F120891
分子式：C36H42ClN3O6
分子量：648.19
分子式：C36H42ClN3O6
分子量：648.19
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
275
In-stock
10mg
440
In-stock
50mg
1560
In-stock
100mg
2320
In-stock
200mg
3120
In-stock
结构图
CAS No: 132866-11-6
产品详情
生物活性：
Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC50 of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research.
体内研究：
Lercanidipine (1, 0.5 与 0.25 mg/kg, 静脉注射, 即刻给药) 可显著降低 MCAo 模型大鼠的神经功能缺损评分、运动功能缺损评分和脑梗死体积。Lercanidipine (1.92-0.12 mg/kg, 口服, 即刻给药) 能有效且剂量依赖性地降低自发性高血压大鼠的血压 。Animal Model:Albino male Wistar rats, middle cerebral artery occlusion (MCAo) model
Dosage:1, 0.5 and 0.25 mg/kg
Administration:Intraperitoneal injection (i.p.), acute administration
Result:Showed neuroprotective effect in focal cerebral ischemic-reperfusion injury model, most effective dose was found to be at 0.5 mg/kg. Significantly attenuated percentage infarct volume, significantly improved the apparent diffusion coefficient. Declined MMP-9 activity significantly in all Lercanidipine treated groups till 240 min post-reperfusion, while MMP-2 activity was inhibited only till 120 min post-reperfusion. Decreased caspase-3 activity significantly in Lercanidipine 15 and 120 min post-reperfusion groups only. Exhibited significant reduction in caspase-9 activity in all groups except at 240 min post-reperfusion group.
Animal Model:Male SHRs
Dosage:1.92, 0.96, 0.48, 0.24 and 0.12 mg/kg
Administration:Oral gavage (p.o.) for once
Result:Increased the AOC values of mean arterial pressure in a dose-dependent manner (285.4 mmHg×hour for 1.92 mg) as well as decreased BP.
体外研究：
Lercanidipine (1, 10 μM, 24 h) 通过下调 iNOS、MMP-2/MMP-9、HMGB1，以及抑制 MAPKs、Akt/IkB-a 和 NF-kB 通路，抑制 LPS/IFN-γ 诱导的 VSMCs 中的 NO、ROS 和 TNF-a。
Lercanidipine is a third-generation, lipophilic, brain-penetrant, vascular-selective and orally active dihydropyridine-calcium channel blocker with a pIC50 of 7.74 (converts from μM). Lercanidipine has long lasting antihypertensive action as well as reno- and neuro-protective effect. Lercanidipine also shows anti-oxidant, anti-inflammatory and anti-apoptotic properties. Lercanidipine can be used in cardiovascular and neurological research.
体内研究：
Lercanidipine (1, 0.5 与 0.25 mg/kg, 静脉注射, 即刻给药) 可显著降低 MCAo 模型大鼠的神经功能缺损评分、运动功能缺损评分和脑梗死体积。Lercanidipine (1.92-0.12 mg/kg, 口服, 即刻给药) 能有效且剂量依赖性地降低自发性高血压大鼠的血压 。Animal Model:Albino male Wistar rats, middle cerebral artery occlusion (MCAo) model
Dosage:1, 0.5 and 0.25 mg/kg
Administration:Intraperitoneal injection (i.p.), acute administration
Result:Showed neuroprotective effect in focal cerebral ischemic-reperfusion injury model, most effective dose was found to be at 0.5 mg/kg. Significantly attenuated percentage infarct volume, significantly improved the apparent diffusion coefficient. Declined MMP-9 activity significantly in all Lercanidipine treated groups till 240 min post-reperfusion, while MMP-2 activity was inhibited only till 120 min post-reperfusion. Decreased caspase-3 activity significantly in Lercanidipine 15 and 120 min post-reperfusion groups only. Exhibited significant reduction in caspase-9 activity in all groups except at 240 min post-reperfusion group.
Animal Model:Male SHRs
Dosage:1.92, 0.96, 0.48, 0.24 and 0.12 mg/kg
Administration:Oral gavage (p.o.) for once
Result:Increased the AOC values of mean arterial pressure in a dose-dependent manner (285.4 mmHg×hour for 1.92 mg) as well as decreased BP.
体外研究：
Lercanidipine (1, 10 μM, 24 h) 通过下调 iNOS、MMP-2/MMP-9、HMGB1，以及抑制 MAPKs、Akt/IkB-a 和 NF-kB 通路，抑制 LPS/IFN-γ 诱导的 VSMCs 中的 NO、ROS 和 TNF-a。
产品资料
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