Clemizole hydrochloride - CAS 1163-36-6
Catalog number: B0084-055145
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C19H20ClN3.HCl
Molecular Weight:
362.30
COA:
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Targets:
Histamine Receptor
Description:
The hydrochloride salt form of clemizole, which is a histamine H1 antagonist with antitumor activity. It also has hepatitis C antiviral effect through restraining NS4B function and could also be used as an anticonvulsant in zebrafish Dravet syndrome model.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-055145 100 mg $198 In stock
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Publication citing BOC Sciences Products
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Purity:
95%
Related CAS:
442-52-4 (free base)
Appearance:
Solid Powder
Synonyms:
Allercur; Clemizole HCl; Clemizole (hydrochloride); Reactrol; 1-[(4-chlorophenyl)methyl]-2-(pyrrolidin-1-ylmethyl)benzimidazole hydrochloride
Solubility:
DMSO: ≥ 3.6 mg/mL
Storage:
-20ºC Freeze
MSDS:
Inquire
Shelf Life:
2 years
Boiling Point:
506.1ºC at 760 mmHg
Density:
1.25 g/cm3
InChIKey:
DNFMJYXRIMLMBZ-UHFFFAOYSA-N
InChI:
InChI=1S/C19H20ClN3.ClH/c20-16-9-7-15(8-10-16)13-23-18-6-2-1-5-17(18)21-19(23)14-22-11-3-4-12-22;/h1-2,5-10H,3-4,11-14H2;1H
Canonical SMILES:
C1CCN(C1)CC2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)Cl.Cl
1.PRURITUS OF DERMATOSES TREATED ADJUNCTIVELY WITH ORAL CLEMIZOLE HYDROCHLORIDE.
OSMENT LS, BROYLES JA. Clin Med (Northfield). 1963 Sep;70:1637-40.
2.Clemizole hydrochloride: a clinical evaluation of its antipruritic effect.
WANSKER BA. Skin (Los Angeles). 1962 Jun;1:157-9.
3.The hepatitis C virus (HCV) NS4B RNA binding inhibitor clemizole is highly synergistic with HCV protease inhibitors.
Einav S1, Sobol HD, Gehrig E, Glenn JS. J Infect Dis. 2010 Jul 1;202(1):65-74. doi: 10.1086/653080.
BACKGROUND: We recently identified a compound, clemizole hydrochloride, that inhibits NS4B's RNA binding and hepatitis C virus (HCV) replication. Although significant, clemizole's antiviral effect is moderate (50% effective concentration of 8 microM against an HCV genotype 2a clone). We hypothesized that the combination of clemizole with other anti-HCV agents can increase the antiviral effect over that achieved with each drug alone and could also decrease the emergence of viral resistance.
4.Discovery of a hepatitis C target and its pharmacological inhibitors by microfluidic affinity analysis.
Einav S1, Gerber D, Bryson PD, Sklan EH, Elazar M, Maerkl SJ, Glenn JS, Quake SR. Nat Biotechnol. 2008 Sep;26(9):1019-27. doi: 10.1038/nbt.1490.
More effective therapies are urgently needed against hepatitis C virus (HCV), a major cause of viral hepatitis. We used in vitro protein expression and microfluidic affinity analysis to study RNA binding by the HCV transmembrane protein NS4B, which plays an essential role in HCV RNA replication. We show that HCV NS4B binds RNA and that this binding is specific for the 3' terminus of the negative strand of the viral genome with a dissociation constant (Kd) of approximately 3.4 nM. A high-throughput microfluidic screen of a compound library identified 18 compounds that substantially inhibited binding of RNA by NS4B. One of these compounds, clemizole hydrochloride, was found to inhibit HCV RNA replication in cell culture that was mediated by its suppression of NS4B's RNA binding, with little toxicity for the host cell. These results yield new insight into the HCV life cycle and provide a candidate compound for pharmaceutical development.
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CAS 1163-36-6 Clemizole hydrochloride

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