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Clemizole hydrochloride

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产品编号 T1822LCas号 1163-36-6
别名 盐酸克立咪唑, 克立咪唑盐酸

Clemizole hydrochloride 是一种 TRPC5通道的抑制剂。它还是一种 H1 组胺受体拮抗剂,抑制 HCV 复制。

Clemizole hydrochloride

Clemizole hydrochloride

Rating icon 很棒
纯度: 99.91%
产品编号 T1822L 别名 盐酸克立咪唑, 克立咪唑盐酸Cas号 1163-36-6

Clemizole hydrochloride 是一种 TRPC5通道的抑制剂。它还是一种 H1 组胺受体拮抗剂,抑制 HCV 复制。

规格价格库存数量
1 mg¥ 185现货
5 mg¥ 413现货
10 mg¥ 662现货
25 mg¥ 993现货
50 mg¥ 1,590现货
100 mg¥ 2,880期货
1 mL x 10 mM (in DMSO)¥ 455现货
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产品介绍

生物活性
产品描述
Clemizole hydrochloride is an antagonist for H1 histamine receptor. According to the research, Clemizole hydrochloride can inhibit hepatitis C virus (HCV) replication and NS4B's RNA binding.
靶点活性
RNA binding by NS4B:24±1 nM, Viral replication:8 µM(EC50)
体外活性
Clemizole hydrochloride is found to inhibit HCV RNA replication in cell culture that is mediated by its suppression of NS4B's RNA binding, with little toxicity for the host cell. The EC50 of Clemizole on the W55R mutant J6/JFH RNA is ~18 μM (2.25 times the EC50 of the wild-type RNA)[1]. Clemizole is a novel inhibitor of TRPC5 channels. Clemizole efficiently blocks TRPC5 currents and Ca2+ entry in the low micromolar range (IC50=1.0-1.3 μM). Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC50=6.4 μM), the closest structural relative of TRPC5, and an almost 10-fold selectivity over TRPC3 (IC50=9.1 μM) and TRPC6 (IC50=11.3 μM). Clemizole hydrochloride as a novel blocker of TRPC5 with a half-maximal inhibitory concentration of 1.1 μM. The concentration-response curves confirmed a concentration-dependent block of TRPC5 by Clemizole and revealed an apparent IC50 of 1.1±0.04 μM[2].
体内活性
Clemizole hydrochloride has an unexpectedly short plasma half-life (measured at 0.15 hours) which is very rapidly biotransformed into a glucuronide (M14) and a dealkylated metabolite (M12) and into a variety of lesser metabolites in C57BL/6J mice[3].
细胞实验
Clemizole hydrochloride is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. Huh7.5 cells are maintained in DMEM supplemented with 1% L-Glutamine, 1% Penicillin, 1% Streptomycin, 1× nonessential amino acids and 10% FBS. Cell lines are passaged twice weekly after treatment with 0.05% trypsin-0.02% EDTA and seeding at a dilution of 1:5. Subconfluent Huh7.5 cells are trypsinized and collected by centrifugation at 700 g for 5 min. The cells are then washed three times in ice-cold RNase-free PBS and resuspended at 1.5×107 cells/mL in PBS. Wild-type or mutant FL-J6/JFH-5′C19Rluc2AUbi RNA for electroporation is generated by transcription of XbaI linearized DNA templates using the T7 MEGAscript kit, followed by purification (RNA transcription and fluorescent labeling). We mixed 5 μg of RNA with 400 μL of washed Huh7.5 cells in a 2-mm-gap cuvette (BTX) and immediately pulsed (0.82 kV, five 99 μs pulses) with a BTX-830 electroporator. After a 10 min recovery at 25°C, pulsed cells are diluted into 10 mL of prewarmed growth medium. Cells from several electroporations are pooled to a common stock and seeded in 6-well plates (5×105 cells per well). After 24 h, medium is replaced and cells are grown in the presence of serial dilutions of the various inhibitory compounds (e.g., Clemizole hydrochloride) identified in the screen. Seventeen commercially available compounds, out of the 18 identified, are analyzed. Untreated cells are used as a negative control for water-soluble compounds. For compounds (e.g., Clemizole hydrochloride) solubilized in DMSO, untreated cells are grown in the presence of corresponding concentrations of the solvent as a negative control. Medium is changed daily. After 72 h of treatment cells are subjected to an Alamar Blue-based viability assay and luciferase assay. After 72 h of treatment cells are incubated for 3 h at 37°C in the presence of 10% Alamar Blue reagent.Plates are then scanned and fluorescence is detected by using FLEXstation II 384. Depending on the inhibitory compound's solvent (e.g., Clemizole hydrochloride), water or DMSO, signal is normalized relatively to untreated samples or samples grown in the presence of DMSO, respectively[1].
别名盐酸克立咪唑, 克立咪唑盐酸
化学信息
分子量362.3
分子式C19H21Cl2N3
CAS No.1163-36-6
SmilesClc1ccc(Cn2c(CN3CCCC3)nc3ccccc23)cc1.Cl
密度1.25 g/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.
溶解度信息
DMSO: 18.11 mg/mL (50 mM)
H2O: 7.25 mg/mL (20 mM)
溶液配制表
H2O/DMSO
1mg5mg10mg50mg
1 mM2.7601 mL13.8007 mL27.6014 mL138.0072 mL
5 mM0.5520 mL2.7601 mL5.5203 mL27.6014 mL
10 mM0.2760 mL1.3801 mL2.7601 mL13.8007 mL
20 mM0.1380 mL0.6900 mL1.3801 mL6.9004 mL
DMSO
1mg5mg10mg50mg
50 mM0.0552 mL0.2760 mL0.5520 mL2.7601 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 20 g ,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% 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 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 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | 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。

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
%ddH2O

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