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Lacidipine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Lacidipine图片
CAS NO:103890-78-4
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议

产品名称
拉西地平
产品介绍
Lacidipine 是一种口服有效的和具有高度选择性的 L 型钙离子通道阻滞剂,作用于平滑肌的钙通道,主要扩张周围动脉,减少外周阻力,具有长效抗高血压活性。Lacidipine 通过调节caspase-3途径来保护 HKCs 免受 ATP 耗尽和恢复所诱发的凋亡。Lacidipine 可用于高血压,动脉粥样硬化和急性肾脏损伤的研究。
生物活性

Lacidipine is an orally active and highly selectiveL-type calcium channelblocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs fromapoptosisinduced by ATP depletion and recovery by modulating thecaspase-3pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI)[1][2].

体外研究
(In Vitro)

Lacidipine (0.01-100 μM; 24 h) inhibits HKCs proliferation in vitro in a concentration-dependent manner[1].
Lacidipine (0.01-100 μM; 24 h) protects HKCs against apoptosis induced by ATP depletion and recovery by regulating the caspase-3 pathway[1].

Cell Proliferation Assay[1]

Cell Line:HKC cells
Concentration:0.01-100 μM
Incubation Time:24 h
Result:Exhibited anti-proliferative activity in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line:HKC cells (renal ischemia reperfusion (I/R) model)
Concentration:1, 10 μM
Incubation Time:24 h
Result:AA-induced HKC cells apoptosis, with proportion of early apoptotic cells of 1.47% and 0.30% for 1 and 10 μM dosage, respectively.

Western Blot Analysis[1]

Cell Line:HKC cells (renal ischemia reperfusion (I/R) model)
Concentration:1, 10 μM
Incubation Time:24 h (pretreat)
Result:Decreased the expression of cyt c of injured cells following ATP depletion and recovery.
Significantly increased the expression of the Bcl-2 protein, but decreased the Bax protein.
体内研究
(In Vivo)

Lacidipine (0.3, 1.0, 3.0 mg/kg; p.o.; single daily for 10 weeks) shows anti-atherogenic effects in the apoE-deficient mouse, and reduces plasma endothelin concentrations[2].

Animal Model:Female C57BL/6 mice (Homozygous; apoE-deficient; atherosclerosis model)[2].
Dosage:0.3, 1.0, 3.0 mg/kg
Administration:Oral gavage; single daily for 10 weeks.
Result:Induced a significant dose-dependent decrease in plasma endothelin levels.
Significantly reduced the mean lesion area in a dose-related manner by 10, 17 and 53% for 0.3, 1.0, 3.0 mg/kg, respectively.
Clinical Trial
分子量

455.54

性状

Solid

Formula

C26H33NO6

CAS 号

103890-78-4

中文名称

拉西地平;司乐平

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL(109.76 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.1952 mL10.9760 mL21.9520 mL
5 mM0.4390 mL2.1952 mL4.3904 mL
10 mM0.2195 mL1.0976 mL2.1952 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40%PEG300   5%Tween-80   45% saline

    Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.49 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (5.49 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (5.49 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。