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顶部相关产品产品介绍化学信息储存和溶解信息计算器

Clemastine

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纯度: 99.21%

货号 T19966Cas号 15686-51-8

别名 氯马斯汀, Mecloprodin, Meclastin, HS-592, HS592, HS 592

Clemastine (Meclastin) 是 H1 受体的拮抗剂，具有抗炎作用。

Clemastine
其他形式的 “Clemastine”:
Clemastine fumarateT014714976-57-9
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Clemastine

一键复制产品信息
Rating icon 很棒

纯度: 99.21%

货号 T19966 别名 氯马斯汀, Mecloprodin, Meclastin, HS-592, HS592, HS 592Cas号 15686-51-8

Clemastine (Meclastin) 是 H1 受体的拮抗剂，具有抗炎作用。

规格价格库存数量
10 mg
¥ 427
现货
25 mg
¥ 686
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50 mg
¥ 996
现货
100 mg
¥ 1,645
现货
1 mL x 10 mM (in DMSO)
¥ 267
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纯度: 99.21%
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产品介绍

生物活性
产品描述
Clemastine (Meclastin) is an antagonist of the H1 receptor and exhibits anti-inflammatory effects.
别名氯马斯汀, Mecloprodin, Meclastin, HS-592, HS592, HS 592
化学信息
分子量343.89
分子式C21H26ClNO
CAS No.15686-51-8
Smiles[C@@](OCC[C@@H]1N(C)CCC1)(C)(C2=CC=C(Cl)C=C2)C3=CC=CC=C3
密度1.31g/cm3
储存&溶解度
存储keep away from moisture | 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
DMSO: 25 mg/mL (72.7 mM), Sonication is recommended.
溶液配制表
DMSO
1mg5mg10mg50mg
1 mM2.9079 mL14.5395 mL29.0791 mL145.3953 mL
5 mM0.5816 mL2.9079 mL5.8158 mL29.0791 mL
10 mM0.2908 mL1.4540 mL2.9079 mL14.5395 mL
20 mM0.1454 mL0.7270 mL1.4540 mL7.2698 mL
50 mM0.0582 mL0.2908 mL0.5816 mL2.9079 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 μL， TargetMol | 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: 取 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： DMSO ， PEG300 / PEG400 ， Tween 80 ， SBE-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

TargetMol AI Summary
Clemastine exhibits a comprehensive range of bioactivities and pharmacokinetic properties. It has a partition coefficient (logD6.5) of 1.65, delta logD value of -0.89, ionization constant (pKa) of 9.2, and an oral bioavailability of 49.0% in humans. Notably, it inhibits the uptake of 4-(4-(dimethylamino)styryl)-N-methylpyridinium at human OCT1 with an IC50 value of 4900.0 nM, showing 78.8% inhibition at a concentration of 100 uM. Bioactivity assays reveal that Clemastine exhibits a moderate potency as an inhibitor of various Cytochrome P450 enzymes (2C19, 2D6, 3A4), as well as displays agonist and antagonist activities across numerous receptors and enzymes. It also inhibits 15-human lipoxygenase 2 and ATXN expression and interacts with a variety of receptors related to cancer cell targeting, genotoxicity, and virus entry inhibition. Specifically, Clemastine shows affinity for histamine H1 central receptors, multiple dopamine receptors (D1-D3), serotonin receptors (5-HT1B, 5-HT2 family, 5-HT6), sigma receptors (Sigma1, Sigma2), as well as adrenergic and muscarinic acetylcholine receptors. Moreover, it has inhibitory activities on human CYP2C19 and CYP3A4, with a varying IC50 ratio depending on the substrate used. In antiviral studies, Clemastine demonstrated activity against Ebolavirus and SARS-CoV-2, inhibiting viral entry and replication with IC50 values of 1100.0 nM and 2137.96 nM, respectively. It also shows significant interactions with enzymes such as HDAC6 and various PDEs, highlighting its broad spectrum of biochemical targets. Despite its bioactivity, Clemastine shows potential hepatotoxicity, indicated by elevated levels of liver enzymes (ALT, AST, ALP) and associated symptoms such as liver damage and cirrhosis but no acute liver toxicity observed. Furthermore, it presents with a logD7.4 value favorable for bioavailability and distribution. Overall, Clemastine's extensive interaction with multiple biological pathways and receptors presents it as a compound of significant pharmacological interest, although caution regarding liver toxicity is advised..
Note: Summary generated by AI, AI may be wrong some times, we do not provide any medical advice and only sell our product to accredited institution, Please cross-check with other sources, data source: chembl

关键词

HistamineReceptorHistamine ReceptorH1 receptorClemastine
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