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  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 是第三代、親脂性、可穿透血腦屏障、血管選擇性、具有口服活性的二氫吡啶鈣通道阻斷劑，pIC50 為 7.74(由 微摩爾濃度 轉(zhuǎn)換而來)。Lercanidipine 具有持久的降壓作用以及腎臟和神經(jīng)保護(hù)作用，還具有抗氧化、抗炎和抗凋亡的特性。Lercanidipine 可用于心血管和神經(jīng)學(xué)研究。

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Lercanidipine Chemical Structure

Lercanidipine Chemical Structure

CAS No. : 100427-26-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥1292
In-stock
5 mg ￥960
In-stock
10 mg   詢價(jià)  
50 mg   詢價(jià)  

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Other Forms of Lercanidipine:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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]
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
LLC-MK2 IC50
434.99 μM
Compound: Lercanidipine
Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Cytotoxicity against rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
[PMID: 20934347]
LLC-MK2 IC50
8.43 μM
Compound: Lercanidipine
Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi infected in rhesus monkey LLC-MK2 cells after 48 hrs by MTT assay
[PMID: 20934347]
體外研究
(In Vitro)

Lercanidipine (1, 10 μM, 24 h) 通過下調(diào) iNOS、MMP-2/MMP-9、HMGB1，以及抑制 MAPKs、Akt/IkB-a 和 NF-kB 通路，抑制 LPS/IFN-γ 誘導(dǎo)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.

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.
體內(nèi)研究
(In Vivo)

Lercanidipine (1, 0.5 與 0.25 mg/kg, 靜脈注射, 即刻給藥) 可顯著降低 MCAo 模型大鼠的神經(jīng)功能缺損評分、運(yùn)動(dòng)功能缺損評分和腦梗死體積[3]。
Lercanidipine (1.92-0.12 mg/kg, 口服, 即刻給藥) 能有效且劑量依賴性地降低自發(fā)性高血壓大鼠的血壓 [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 號(hào)
性狀

固體

顏色

Light yellow to yellow

中文名稱

樂卡地平
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式

4°C, protect from light

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

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 100 mg/mL (163.47 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

以下溶解方案源自文獻(xiàn)，僅供參考，建議您先取少量樣品進(jìn)行嘗試。

  • 方案 一

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

動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料

純度: 99.65%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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.

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產(chǎn)品名稱：
Lercanidipine
目錄號(hào)：
HY-B0612
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