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Ticlopidine

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纯度: 99.67%

货号 T4190Cas号 55142-85-3

别名 噻氯匹定, Ticlid, PCR 5332

Ticlopidine (PCR 5332) 是抗血栓前药。它是CYP2C19人肝细胞色素的抑制剂,抑制 CYP2C9 及 CYP3A4。他是变构CD39的非竞争性抑制剂,能够阻断 NTPDase 同工酶,对NTPDase2和NTPDase3的IC50分别为 170 µM 和 149 µM。

Ticlopidine
其他形式的 “Ticlopidine”:

Ticlopidine

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Rating icon 很棒

纯度: 99.67%

货号 T4190 别名 噻氯匹定, Ticlid, PCR 5332Cas号 55142-85-3

Ticlopidine (PCR 5332) 是抗血栓前药。它是CYP2C19人肝细胞色素的抑制剂,抑制 CYP2C9 及 CYP3A4。他是变构CD39的非竞争性抑制剂,能够阻断 NTPDase 同工酶,对NTPDase2和NTPDase3的IC50分别为 170 µM 和 149 µM。

规格价格库存数量
5 mg
¥ 235
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10 mg
¥ 343
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25 mg
¥ 663
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50 mg
¥ 970
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100 mg
¥ 1,490
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500 mg
¥ 3,720
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纯度: 99.67%
颜色: 白色
性状: Solid
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产品介绍


Ticlopidine AI Summary
Ticlopidine exhibits a diverse range of bioactivities, primarily pertaining to its antithrombotic and inhibitory effects on various enzymes and receptors. It demonstrates significant antiplatelet activity by inhibiting collagen and ADP-induced platelet aggregation in both human and rabbit platelet-rich plasma (PRP). Notably, it has an IC50 value of 3180.0 nM against ADP-induced aggregation in rabbits and exhibits inhibitory activities against thrombin-induced platelet aggregation with an IC50 of 1550000.0 nM. In mouse models, Ticlopidine shows an ID50 of 260.0 mg/kg for preventing acute thrombic death induced by collagen. The effective doses (ED50) for antithrombotic activity are 151.64 umol/kg-1 and 40.0 mg/kg-1 in mice. Additionally, it demonstrates high in vivo antithrombotic activity with a PD50 of 120.0 mg/kg and significant inhibition in collagen-induced assays in rats. The compound also shows substantial inhibitory effects on several cytochrome P450 enzymes, including CYP2B6, CYP2C19, CYP3A4, and others, indicating potential drug-drug interaction concerns. It has a Ki value of 200.0 nM for CYP2B6 and demonstrates time-dependent inhibition of CYP2C19 with a Ki of 3300.0 nM and a Kinact of 0.07 min-1. The compound also strongly inhibits human liver microsomal enzymes, with IC50 values of 210.0 nM and 70000.0 nM for CYP2B6 and CYP2C19, respectively. In terms of liver toxicity, Ticlopidine is associated with significant risk, exhibiting a Drug-Induced Liver Injury (DILI) severity score of 4.0. It shows moderate to high hepatotoxicity in markers such as ALT, ALP, AST, and others, contributing to its cytolytic and cholestatic liver toxicity profiles in clinical settings. Additionally, Ticlopidine demonstrates antiviral activity against SARS-CoV-2 and possesses antimicrobial properties, particularly against methicillin-resistant Staphylococcus aureus (MRSA). It shows moderate efficacy in reducing the minimum inhibitory concentration (MIC) and has potential as a therapeutic agent in infectious diseases. Overall, Ticlopidine has demonstrated a broad spectrum of bioactivities, making it a candidate for further pharmacological exploration while also presenting considerations for safety and interaction profiles..
Note: Summary generated by AI. Data source: ChEMBL
生物活性
产品描述
Ticlopidine (PCR 5332) is an antiplatelet drug in the thienopyridine family which is an adenosine diphosphate (ADP) receptor inhibitor.
别名噻氯匹定, Ticlid, PCR 5332
化学信息
分子量263.79
分子式C14H14ClNS
CAS No.55142-85-3
SmilesClc1ccccc1CN1CCc2sccc2C1
密度1.273 g/cm3 (Predicted)
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: 55 mg/mL (208.5 mM), Sonication is recommended.
H2O: Insoluble
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM3.7909 mL18.9545 mL37.9089 mL189.5447 mL
5 mM0.7582 mL3.7909 mL7.5818 mL37.9089 mL
10 mM0.3791 mL1.8954 mL3.7909 mL18.9545 mL
20 mM0.1895 mL0.9477 mL1.8954 mL9.4772 mL
50 mM0.0758 mL0.3791 mL0.7582 mL3.7909 mL
100 mM0.0379 mL0.1895 mL0.3791 mL1.8954 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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