Clemizole

Catalog No.S6410

Clemizole Chemical Structure

Molecular Weight(MW): 325.84

Clemizole, a first-generation histamine receptor (H1) 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 TRPC5 ion channels.

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Biological Activity

Description Clemizole, a first-generation histamine receptor (H1) 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 TRPC5 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[3].

In vivo

Clemizole is rapidly metabolized in mice with a plasma half-life of <10 min (compared to 3.4 h in humans), limiting its evaluation in murine models[2].

Protocol

Solubility (25°C)

In vitro DMSO 65 mg/mL (199.48 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 325.84
Formula

C19H20ClN3

CAS No. 442-52-4
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID