[CAS NO. 442-52-4] Clemizole

Name: Clemizole
Brand: Arctom Scientific
SKU: SLK-S6410

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PRODUCTS SPECIFICATIONS [442-52-4]

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Catalog

SLK-S6410

Brand

Selleck

CAS

442-52-4

DESCRIPTION [442-52-4]

Overview

MDL	-
Molecular Weight	325.84
Molecular Formula	C19H20ClN3
SMILES	C(N1C=2C(N=C1CN3CCCC3)=CC=CC2)C4=CC=C(Cl)C=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	3.0690 mL	15.3450 mL	30.6899 mL
5 mM	0.6138 mL	3.0690 mL	6.1380 mL
10 mM	0.3069 mL	1.5345 mL	3.0690 mL
50 mM	0.0614 mL	0.3069 mL	0.6138 mL

Description

Clemizole, a first-generation antagonist, is a potent inhibitor of behavioural and electrographic seizure activity. It has a potential therapeutic effect on hepatitis C infection and also potently inhibits ion channels.

Targets

H1 receptor ^[1]

TRPC5 ^[3]

In vitro

Clemizole efficiently blocks TRPC5 currents and Ca2+ entry in the low micromolar range (IC50 = 1.0-1.3 μM), as determined by fluorometric [Ca2+]I measurements and patch clamp recordings. Based on fluorometric [Ca2+]i measurements, clemizole exhibits a 6-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). TRPM3 and M8 as well as TRPV1, V2, V3 and V4 channels are only weakly affected by markedly higher clemizole concentrations. Clemizole is not only effective in blocking heterologously expressed TRPC5 homomers but also TRPC1:TRPC5 heteromers as well as native TRPC5-like currents in the U-87 glioblastoma cell line.

References

[1] Aliesha Griffin, et al. Brain. 2017, 140(3): 669–683.
[2] Nishimura T, et al. J Pharmacol Exp Ther. 2013, 344(2):388-96.
[3] Richter JM, et al. Mol Pharmacol. 2014, 86(5):514-21.

Synonyms

1H-Benzimidazole, 1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-

Benzimidazole, 1-(p-chlorobenzyl)-2-(1-pyrrolidinylmethyl)-

Pyrrolidine, 1-[(1-p-chlorobenzyl-2-benzimidazolyl)methyl]-

1-[(4-Chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole

1-p-Chlorobenzyl-2-pyrrolidino-methylbenzimidazole

1-p-Chlorobenzyl-2-(1-pyrrolidinylmethyl)benzimidazole

1-(p-Chlorobenzyl)-2-pyrrolidylmethylenebenzimidazole

Histacur

Histakool

Clemizole

Lergopenin

Depocural

NSC 46261