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. |
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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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(109.76 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 2.1952 mL | 10.9760 mL | 21.9520 mL | | 5 mM | 0.4390 mL | 2.1952 mL | 4.3904 mL | | 10 mM | 0.2195 mL | 1.0976 mL | 2.1952 mL |
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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。 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。
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