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Amlodipine
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很棒纯度: 99.60%
货号 T1385Cas号 88150-42-9
别名 氨氯地平, UK-48340
Amlodipine (UK-48340) 是可口服的二氢吡啶钙通道阻滞剂，有抗心绞痛作用。它通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流，用于高血压和癌症的研究。
其他形式的 “Amlodipine”:
Amlodipine
一键复制产品信息 很棒纯度: 99.60%
货号 T1385 别名 氨氯地平, UK-48340Cas号 88150-42-9
Amlodipine (UK-48340) 是可口服的二氢吡啶钙通道阻滞剂，有抗心绞痛作用。它通过阻断电压依赖性的 L 型钙通道，从而抑制钙离子内流，用于高血压和癌症的研究。
| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 50 mg | ¥ 145 | 现货 | |
| 100 mg | ¥ 192 | 现货 | |
| 500 mg | ¥ 415 | 现货 | |
| 1 g | ¥ 591 | 现货 | |
| 5 g | ¥ 1,430 | 现货 |
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产品介绍
Amlodipine AI Summary
Amlodipine demonstrates multifaceted pharmacological and pharmacokinetic profiles. It acts as an in vitro calcium channel antagonist, showing high potency against calcium-induced contractions in potassium-depolarized rat aorta with IC50 values from 1.995 nM to 1584.89 nM and a notable IC50 of 7.943 nM. It also induces a negative inotropic effect on Langendorff-perfused guinea pig heart with a pIC25 of 7.2 and exhibits significant bioactivity in terms of IC50 values, including binding affinities to several adrenergic receptors and the L-type calcium channel. The compound has shown bioactivities such as antihypertensive effects in spontaneously hypertensive rats with an IC50 value of 2.5 nM, and antileishmanial activities against Leishmania donovani.
Pharmacokinetic evaluations in dogs reveal a plasma clearance rate of 11.0 mL.min-1.kg-1, volume of distribution at 25.0 L.kg-1, and a half-life of 30.0 hours. Human pharmacokinetics indicate a similar plasma clearance rate of 7.0 mL.min-1.kg-1, volume of distribution of 17.0 L.kg-1, and a half-life of 34.0 hours. The compound displays a high oral bioavailability of 79.0%, strong protein binding affinity of 98.09%, and a moderate lipophilicity with log P and log D values around 1.55 to 3.3.
Amlodipine inhibits several key enzymes, such as the L-type calcium channel with various IC50 values, TREK-1 channel at 400.0 nM, and human BSEP at 16000.0 nM. It also demonstrates significant antiviral activity against SARS-CoV-2, with an impressive inhibition rate of 94.32% at 10 uM concentration and some inhibitory activity on the SARS-CoV-2 3CL-Pro protease. Additionally, it has shown moderate inhibition of fungal growth and bacterial activities, albeit with lower efficacy against certain pathogens.
The compound has also exhibited hepatotoxicity potential, indicated by relevant liver enzyme increases in various assays. Collectively, these characteristics underscore Amlodipine’s potential for diverse therapeutic applications subject to further evaluations on safety, efficacy, and selectivity..
Note: Summary generated by AI. Data source: ChEMBL 
生物活性
化学信息
储存&溶解度
| 产品描述 | Amlodipine (UK-48340) is a synthetic dihydropyridine and a calcium channel blocker with antihypertensive and antianginal properties. |
| 体外活性 | 在Ang II灌注大鼠中,Amlodipine可显着降低动脉肥厚,内皮功能紊乱.在自发性高血压大鼠中,Amlodipine能够改善心血管肥大和内皮功能障碍. |
| 体内活性 | 在大冠状动脉和主动脉中,Amlodipine增加的亚硝酸盐产生。在细胞内,Amlodipine通过减弱KCl去极化,引起神经元Ca2 +升高。 |
| 别名 | 氨氯地平, UK-48340 |
| 分子量 | 408.88 |
| 分子式 | C20H25ClN2O5 |
| CAS No. | 88150-42-9 |
| Smiles | OS(=O)(=O)C1=CC=CC=C1.CCOC(=O)C1=C(COCCN)NC(C)=C(C1C1=CC=CC=C1Cl)C(=O)OC |
| 密度 | 1.227 g/cm3 (Predicted) |
| 存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| 溶解度信息 | DMSO: 90 mg/mL (220.11 mM), Sonication is recommended.  Ethanol: 76 mg/mL (185.87 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| 体内实验配方 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2.5 mg/mL (6.11 mM), Sonication is recommended. 请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。 | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
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计算器
体内实验配液计算器
请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：
比如您的给药剂量是10 mg/kg，每只动物体重20g，给药体积100 μL， 一共给药动物10只，您使用的配方为5%
DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O， 那么您的工作液浓度为2mg/mL。 以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。
剂量转换
对于不同动物的给药剂量换算，您也可以参考 更多
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