2. Membrane Transporter/Ion Channel Neuronal Signaling Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation MAPK/ERK Pathway
  3. Calcium Channel Apoptosis Reactive Oxygen Species p38 MAPK NF-κB
  4. Lercanidipine

Lercanidipine  (Synonyms: 乐卡地平)

目录号: HY-B0612 纯度: 99.65%
COA 产品使用指南

摩尔计算器

Lercanidipine 是第三代、亲脂性、可穿透血脑屏障、血管选择性、具有口服活性的二氢吡啶钙通道阻断剂，pIC50 为 7.74(由 微摩尔浓度 转换而来)。Lercanidipine 具有持久的降压作用以及肾脏和神经保护作用，还具有抗氧化、抗炎和抗凋亡的特性。Lercanidipine 可用于心血管和神经学研究。

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Lercanidipine Chemical Structure

Lercanidipine Chemical Structure

CAS No. : 100427-26-7

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1292
In-stock
5 mg ￥960
In-stock
10 mg   询价  
50 mg   询价  

* Please select Quantity before adding items.

Lercanidipine 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

查看 Calcium Channel 亚型特异性产品:

查看所有亚型
N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1][2][3][4][5].

IC50 & Target

calcium channel[1]
体外研究
(In Vitro)

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[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Lercanidipine 相关抗体:

Western Blot Analysis[3]

Cell Line: LPS/IFN-γ-induced VSMC
Concentration: 1 and 10 μM
Incubation Time: 24 h
Result: Down-regulated LPS/IFN-γ-induced iNOS, MMP-2/-9, NF-kB expression and IkB-a phosphorylation. Decreased cytosolic HMGB1 fraction and extracellular HMGB1 release while increasing nuclear HMGB1 fraction.
体内研究
(In Vivo)

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[3]。
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 [4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Albino male Wistar rats, middle cerebral artery occlusion (MCAo) model[3]
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 [4]
Dosage: 1.92, 0.96, 0.48, 0.24 and 0.12 mg/kg
Administration: Oral gavage (p.o.), acute administration
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.
Clinical Trial
分子量

611.73

Formula

C36H41N3O6
CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

乐卡地平
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (163.47 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6347 mL 8.1735 mL 16.3471 mL
5 mM 0.3269 mL 1.6347 mL 3.2694 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

以下溶解方案源自文献，仅供参考，建议您先取少量样品进行尝试。

  • 方案 一

    dissolve in 20% ethanol, 20% DMSO and 60% normal saline

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: 99.65%

COA (197 KB) HNMR (291 KB) LCMS (94 KB)

产品使用指南 (1538 KB)
参考文献

Lercanidipine 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6347 mL 8.1735 mL 16.3471 mL 40.8677 mL
5 mM 0.3269 mL 1.6347 mL 3.2694 mL 8.1735 mL
10 mM 0.1635 mL 0.8174 mL 1.6347 mL 4.0868 mL
15 mM 0.1090 mL 0.5449 mL 1.0898 mL 2.7245 mL
20 mM 0.0817 mL 0.4087 mL 0.8174 mL 2.0434 mL
25 mM 0.0654 mL 0.3269 mL 0.6539 mL 1.6347 mL
30 mM 0.0545 mL 0.2725 mL 0.5449 mL 1.3623 mL
40 mM 0.0409 mL 0.2043 mL 0.4087 mL 1.0217 mL
50 mM 0.0327 mL 0.1635 mL 0.3269 mL 0.8174 mL
60 mM 0.0272 mL 0.1362 mL 0.2725 mL 0.6811 mL
80 mM 0.0204 mL 0.1022 mL 0.2043 mL 0.5108 mL
100 mM 0.0163 mL 0.0817 mL 0.1635 mL 0.4087 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lercanidipine100427-26-7乐卡地平Calcium ChannelApoptosisReactive Oxygen Speciesp38 MAPKNF-κBCa2+ channelsCa channelsNuclear factor-κBNuclear factor-kappaBanti-oxidantanti-inflammatoryanti-apoptoticanti-hypertensiveCalcium channel blockerrenoprotectiveneuroprotectivestrokeMCAo modelVSMCSHRInhibitorinhibitorinhibit

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