首页 工具
登录
购物车
Clemizole hydrochloride

Clemizole hydrochloride

产品编号 T1822L   CAS 1163-36-6
别名: 克立咪唑盐酸, 盐酸克立咪唑

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。

TargetMol的所有产品和服务仅用于科学研究,不能被用于人体,我们也不向个人提供产品和服务。
Clemizole hydrochloride Chemical Structure
Clemizole hydrochloride, CAS 1163-36-6
规格 价格/CNY 货期 数量
1 mg ¥ 185 现货
5 mg ¥ 413 现货
10 mg ¥ 663 现货
25 mg ¥ 1,320 现货
50 mg ¥ 2,460 现货
100 mg ¥ 3,910 待询
1 mL * 10 mM (in DMSO) ¥ 455 现货
其他形式的 Clemizole hydrochloride:
产品目录号及名称: Clemizole hydrochloride (T1822L)
点击图片重新获取验证码
选择批次  
纯度: 99.91%
更多批次查询请联系客服
生物活性
化学信息
存储 & 溶解度
参考文献
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 克立咪唑盐酸, 盐酸克立咪唑
分子量 362.3
分子式 C19H21Cl2N3
CAS No. 1163-36-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 18.11 mg/mL (50 mM)

H2O: 7.25 mg/mL (20 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.7601 mL 13.8007 mL 27.6014 mL 69.0036 mL
5 mM 0.552 mL 2.7601 mL 5.5203 mL 13.8007 mL
10 mM 0.276 mL 1.3801 mL 2.7601 mL 6.9004 mL
20 mM 0.138 mL 0.69 mL 1.3801 mL 3.4502 mL
DMSO 50 mM 0.0552 mL 0.276 mL 0.552 mL 1.3801 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
=
X
X
X
=
X
=
/
g/mol

输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Einav S, et al. Discovery of a hepatitis C target and its pharmacological inhibitors by microfluidic affinity analysis. Nat Biotechnol. 2008 Sep;26(9):1019-27. 2. Richter JM, et al. Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5. Mol Pharmacol. 2014 Nov;86(5):514-21. 3. Nishimura T, et al. Using chimeric mice with humanized livers to predict human drug metabolism and a drug-drug interaction. J Pharmacol Exp Ther. 2013 Feb;344(2):388-96.
Dimethindene OXOMEMAZINE Marmin Benztropine mesylate Cetirizine D8 Asenapine Lidocaine 4'-O-Methylnyasol

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌上市药物库 抗癌活性化合物库 抗癌临床化合物库 神经递质受体化合物库 上市药物库 抗病毒库 免疫/炎症分子化合物库 抗肥胖化合物库 临床期小分子药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

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5% 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 μL DMSO (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 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步: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
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Clemizole hydrochloride 1163-36-6 GPCR/G Protein Immunology/Inflammation Microbiology/Virology Neuroscience Proteases/Proteasome HCV Protease Histamine Receptor TRP Channel Transient receptor potential channels 克立咪唑盐酸 Hepatitis C virus Inhibitor Clemizole Hydrochloride inhibit Clemizole 盐酸克立咪唑 HCV inhibitor

 

陶术
生物
TargetMol®中国区唯一合作伙伴
点击进入陶术生物官网陶术生物
联系我们
400-820-0310

上海市静安区江场三路238号8楼