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Clopidogrel

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纯度: 98.83%

货号 T0182Cas号 113665-84-2

别名 氯吡格雷, SR-25990C, (S)-Clopidogrel

Clopidogrel (SR-25990C) 是一种 P2Y12 受体拮抗剂,可降低血小板聚集,用于抑制冠状动脉疾病、周围血管疾病和脑血管疾病中的血凝块。

Clopidogrel

Clopidogrel

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Rating icon 很棒

纯度: 98.83%

货号 T0182 别名 氯吡格雷, SR-25990C, (S)-ClopidogrelCas号 113665-84-2

Clopidogrel (SR-25990C) 是一种 P2Y12 受体拮抗剂,可降低血小板聚集,用于抑制冠状动脉疾病、周围血管疾病和脑血管疾病中的血凝块。

规格价格库存数量
50 mg
¥ 298
现货
100 mg
¥ 418
现货
500 mg
¥ 997
现货
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产品介绍


Clopidogrel AI Summary
Clopidogrel is a multifaceted bioactive substance demonstrating significant inhibitory, modulatory, and cytotoxic properties across various biological targets. It acts as a potent inhibitor of human recombinant carboxylesterase 1 (CES1) with a Km value of 55700 nM and a pKm value of 4.25. In the field of enzymatic inhibition, it also shows mechanism-based inhibition of cytochrome P450 2B6, with Ki values of 500 nM and 1100 nM and Kinact values of 0.35 min^-1 and 0.15 min^-1, respectively. It has considerable activity against the serotonin transporter (SERT), with an IC50 of 562 nM and a Ki of 299 nM. The compound exhibits noteworthy bioactivity in various assays: - It inhibits the Influenza NS1 protein function with a potency of 19952.6 nM. - It demonstrates delayed death inhibition of the malarial parasite plastid with potencies of 8275.3 nM (96-hour incubation) and 11689.1 nM (48-hour incubation). - It functions as an inhibitor of HP1-beta chromodomain interactions with methylated histone tails with a potency of 89125.1 nM. Furthermore, Clopidogrel exhibits pharmacokinetic properties in Sprague-Dawley rats, with a maximum concentration (Cmax) of 21.53 nM reached at 0.583 hours post-administration, a half-life of 2.48 hours, and an area under the curve (AUC) of 32200 ng.hr.mL^-1. It shows a high clearance rate in human liver microsomes exceeding 300 mL.min^-1.g^-1, indicating rapid metabolism. In antiplatelet and antithrombotic assays, the compound effectively inhibits ADP-induced platelet aggregation in rabbit platelets and demonstrates significant antithrombotic activity in rodent models, reducing thrombus weight by 67% in the FeCl2-induced thrombosis model. Additionally, it prolongs bleeding time in various animal models, indicative of its anticoagulant potential. On the toxicity front, Clopidogrel has shown moderate hepatotoxicity, as evidenced by elevated serum ALT and AST enzyme levels, and significant impacts on hepatotoxicity indices. It also shows intravital toxicity by prolonging mesenteric and cuticle bleeding time in rat models. The compound exhibits broad-spectrum antibacterial activity, particularly against methicillin-resistant Staphylococcus aureus (MRSA) USA300, and antifungal activity against Candida albicans and Cryptococcus neoformans. However, its antiviral activity against SARS-CoV-2 is limited, with low inhibition efficacy. Overall, Clopidogrel’s diverse bioactivities suggest its potential as a valuable candidate in pharmaceutical research while underscoring the necessity for careful evaluation of its pharmacodynamics and toxicological profiles in further studies..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Clopidogrel (SR-25990C), a P2Y12 receptor antagonist, decreases platelet aggregation.
别名氯吡格雷, SR-25990C, (S)-Clopidogrel
化学信息
分子量321.82
分子式C16H16ClNO2S
CAS No.113665-84-2
SmilesCOC(=O)[C@@H](N1CCc2sccc2C1)c1ccccc1Cl
密度1.317g/cm3
储存&溶解度
存储Pure form: -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
H2O: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 40 mg/mL (124.29 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.21 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
DMSO
1mg5mg10mg50mg
1 mM3.1073 mL15.5366 mL31.0733 mL155.3664 mL
5 mM0.6215 mL3.1073 mL6.2147 mL31.0733 mL
10 mM0.3107 mL1.5537 mL3.1073 mL15.5366 mL
20 mM0.1554 mL0.7768 mL1.5537 mL7.7683 mL
50 mM0.0621 mL0.3107 mL0.6215 mL3.1073 mL
100 mM0.0311 mL0.1554 mL0.3107 mL1.5537 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 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:
TargetMol | Animal experiments 比如您的给药剂量是10 mg/kg,每只动物体重20g,给药体积100 μLTargetMol | Animal experiments 一共给药动物10只,您使用的配方为5%TargetMol | reagent DMSO + 30%PEG300 + 5%Tween 80 + 60%Saline/PBS/ddH2O, 那么您的工作液浓度为2mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween80, 混匀澄清,再加 600μLSaline/PBS/ddH2OTargetMol | reagent 混匀澄清

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。

方案所需的各类助溶剂如: DMSOPEG300 / PEG400Tween 80SBE-β-CD玉米油 等, 均可在TargetMol网站点击购买。
1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

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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