An antihistamine and TRPC5 channel blocker
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Clemizole (hydrochloride)

Item No. 17695

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[(4-chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole, monohydrochloride
CAS Number
1163-36-6
Synonyms
  • AL 20
  • Allercur
Molecular Formula
C19H20ClN3 • HCl
Formula Weight
362.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 10 mg/mlDMSO:PBS(pH 7.2) (1:2): 0.3 mg/mlEthanol: 2 mg/ml
λmax
205, 252, 276, 283 nm
SMILES
ClC(C=C1)=CC=C1CN2C(CN3CCCC3)=NC4=CC=CC=C42.Cl
InChi Code
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
InChi Key
DNFMJYXRIMLMBZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    Clemizole is an antihistamine that antagonizes the histamine 1 receptor at high nanomolar concentrations.1,2 It less potently blocks transient receptor potential canonical channel 5 (TRPC5; IC50 = 1.0-1.3 µM), with at least 6-fold selectivity for TRPC5 over other TRP channels.3 Clemizole also has hepatitis C antiviral action through inhibition of NS4B function, showing synergy with boceprevir (Item No. 18379), and it inhibits seizures in a zebrafish model of Dravet Syndrome.4,5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Aguilar, M.J., Morales-Olivas, F.J., and Rubio, E. Pharmacological investigation into the effects of histamine and histamine analogues on guinea-pig and rat colon in vitro. Brit. J. Pharmacol. 88(3), 501-506 (1986).

    2. Cortijo, J., Sanz, C., Perpiña, M., et al. Responses to histamine and selective H2-receptor agonists in lung parenchymal strips from normal and sensitized guinea-pigs. Agents Actions 28(1-2), 45-52 (1989).

    3. Richter, J.M., Schaefer, M., and Hill, K. Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5. Mol. Pharmacol. 86(5), 514-521 (2014).

    4. Einav, S., Sobol, H.D., Gehrig, E., et al. The hepatitis C virus (HCV) NS4B RNA binding inhibitor clemizole is highly synergistic with HCV protease inhibitors. J. Infect. Dis. 202(1), 65-74 (2010).

    5. Baraban, S.C., Dinday, M.T., and Hortopan, G.A. Drug screening in Scn1a zebrafish mutant identifies clemizole as a potential Dravet syndrome treatment. Nat. Commun. 4:2410, (2013).