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Cariporide

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纯度: 99.88%

货号 T2238Cas号 159138-80-4

别名 卡立泊来德, HOE-642

Cariporide (HOE-642) 是一种选择性的Na+/H+交换抑制剂。

Cariporide
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Cariporide

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Rating icon 很棒

纯度: 99.88%

货号 T2238 别名 卡立泊来德, HOE-642Cas号 159138-80-4

Cariporide (HOE-642) 是一种选择性的Na+/H+交换抑制剂。

规格价格库存数量
2 mg
¥ 279
现货
5 mg
¥ 438
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10 mg
¥ 627
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25 mg
¥ 1,090
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50 mg
¥ 1,630
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100 mg
¥ 2,420
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500 mg
¥ 5,730
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1 mL x 10 mM (in DMSO)
¥ 443
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产品介绍


Cariporide AI Summary
Cariporide exhibits diverse bioactivities, primarily targeting the sodium/hydrogen exchanger (NHE) family, with potent inhibition of NHE1 (IC50 of 30.0 nM) and moderate inhibition of NHE2 (IC50 of 4300.0 nM). It shows weak activity against NHE3 and NHE5 (IC50 ≥ 1000.0 nM and >30000.0 nM, respectively). It effectively inhibits NHE1-mediated intracellular pH recovery in various cell types, including rat and human platelets, and acidified rabbit erythrocytes. The compound also demonstrates significant cardioprotective effects, reducing myocardial infarct size and improving heart function in ischemia-reperfusion injury models in rats and guinea pigs. Additionally, it shows efficacy in mitigating serum creatine kinase levels and left ventricular end diastolic pressure during ischemic conditions. Pharmacokinetically, Cariporide has an oral bioavailability of 37.0% in rats, a volume of distribution at steady state of 1.3 L/kg, and a mean residence time of 0.4 hours post-intravenous administration. It exhibits a high clearance rate (82% relative to hepatic blood flow). Further, Cariporide shows modest inhibitory activity against SARS-CoV-2, including its 3CL-Pro protease, with inhibition percentages around 13-14% at 20 µM concentration. Lastly, it demonstrates potential inhibitory effects on human HDAC6, shown by inhibition percentages in enzymatic assays with peptide substrates. Overall, Cariporide holds promise for cardiovascular and antiviral therapeutic applications..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Cariporide (HOE-642) (HOE-642), an effective NHE1 inhibitor, has inhibitory effects on the degranulation of human platelets, the formation of platelet-leukocyte-aggregates, and the activation of the GPIIb/IIIa receptor (PAC-1).
靶点活性
NHE1:30 nM
别名卡立泊来德, HOE-642
化学信息
分子量283.35
分子式C12H17N3O3S
CAS No.159138-80-4
SmilesCC(C)c1ccc(cc1S(C)(=O)=O)C(=O)N=C(N)N
密度1.34g/cm3
储存&溶解度
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: 250 mg/mL (882.3 mM), Sonication is recommended.
体内实验配方
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (7.06 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 mM3.5292 mL17.6460 mL35.2920 mL176.4602 mL
5 mM0.7058 mL3.5292 mL7.0584 mL35.2920 mL
10 mM0.3529 mL1.7646 mL3.5292 mL17.6460 mL
20 mM0.1765 mL0.8823 mL1.7646 mL8.8230 mL
50 mM0.0706 mL0.3529 mL0.7058 mL3.5292 mL
100 mM0.0353 mL0.1765 mL0.3529 mL1.7646 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:
比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL, 一共给药动物10只,您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH2O, 那么您的工作液浓度为2 mg/mL
母液配置方法:2 mg 药物溶于 100 μL DMSO ( 母液浓度为 20 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:100 μL DMSO 母液, 添加 400 μL PEG300 混匀澄清, 再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH2O 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: DMSOPEG300PEG400Tween 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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