克立咪唑盐酸盐 - CAS:1163-36-6 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	克立咪唑盐酸盐促销
英文名称:	Clemizole HCl
别名:	克立咪唑盐酸盐 AL-20 HCL;Reactrol HCL;1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)-1H-benzo[d]imidazole hydrochloride
CAS No:	1163-36-6	分子式:	C₁₉H₂₀ClN₃^.HCl	分子量:	362.3
CAS No:	1163-36-6
分子式:	C₁₉H₂₀ClN₃^.HCl
分子量:	362.3
EINEC:	214-605-4
EINEC:	214-605-4

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C10370 克立咪唑盐酸盐 ≥98%(HPLC) (psaitong)

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包装规格：

5mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO(≥3mg/mL)

产品描述：

基本信息

产品编号：	C10370
产品名称：	Clemizole HCl
CAS:	1163-36-6	储存条件	粉末	-20℃	四年

分子式：	C19H20ClN3.HCl		溶于液体	-80℃	6个月
分子量：	362.30			-20℃	1个月
化学名：	1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)-1H-benzo[d]imidazole hydrochloride
Solubility (25°C)：
体外:	DMSO
	Ethanol
	Water
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.7601mL	13.8007mL	27.6014mL
5mM	0.5520mL	2.7601mL	5.5203mL
10mM	0.2760mL	1.3801mL	2.7601mL

生物活性

产品描述	一种H1组胺受体(H1 histamine receptor)拮抗剂，抑制HCV复制。
靶点	IC50:24nM (NS4B) H1 histamine receptor
体外研究	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 ~18µM (2.25 times the EC50 of the wild-type RNA).Clemizole is a novel inhibitor of TRPC5 channels.Clemizole efficiently blocks TRPC5 currents and Ca2+entry in the low micromolar range (IC50=1.0-1.3µM).Clemizole exhibits a six-fold selectivity for TRPC5 over TRPC4β (IC50=6.4µM),the closest structural relative of TRPC5,and an almost 10-fold selectivity over TRPC3 (IC50=9.1µM) and TRPC6 (IC50=11.3µM).Clemizole hydrochloride as a novel blocker of TRPC5 with a half-maximal inhibitory concentration of 1.1µM.The concentration-response curves confirmed a concentration-dependent block of TRPC5 by AClemizole and revealed an apparent IC50 of 1.1±0.04µM.
体内研究	Clemizole hydrochloride has an unexpectedly short plasma half-life (measured at 0.15 hours);it is very rapidly biotransformed into a glucuronide (M14) and a dealkylated metabolite (M12) and into a variety of lesser metabolites in C57BL/6J mice.

推荐实验方法(仅供参考)

细胞实验:

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 700g 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 FLJ6/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 5µg of RNA with 400µL of washed Huh7.5 cells in a 2-mm-gap cuvette (BTX) and immediately pulsed (0.82 kV,five 99µs pulses) with a BTX-830 electroporator.After a 10 min recovery at 25℃,pulsed cells are diluted into 10mL 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 24h,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 72h of treatment cells are subjected to an Alamar Blue-based viability assay and luciferase assay.After 72h of treatment cells are incubated for 3 h at 37℃ 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.

动物实验:

Mice

Eight control NOG mice and eight humanized TK-NOG mice are administered 25mg/kg by mouth Clemizole,and blood samples are collected 30 minutes after administration.The C57BL/6J mice (3 per time point) are given 25mg/kg by mouth clemizole,and blood samples are collected for analysis at 15 and 30 minutes and 1,2,4,and 6 hours after administration.For the DDI studies,eight humanized TK-NOG mice are given Clemizole (25mg/kg by mouth) with or without Ritonavir (20mg/kg by mouth), and blood samples are collected 30 minutes after administration.Six of these mice are also treated with Debrisoquine (10mg/kg by mouth) in the presence or absence of Ritonavir (20mg/kg by mouth),and plasma samples are obtained 2 hours later for analysis.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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