Home Neuronal Signaling TRP Channel inhibitor - Dopamine Receptor antagonist Clemizole For research use only.

Clemizole

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.

Clemizole Chemical Structure

Clemizole Chemical Structure

CAS: 442-52-4

Purity & Quality Control

Batch: S641001 DMSO] 65 mg/mL] false] ] ] false] ] ] false Purity: 99.67%
99.67

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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
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
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].
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03069508 Unknown status
Hepatocellular Carcinoma
Eiger Group International Inc.
 February 13 2017 Phase 2
NCT00945880 Completed
Hepatitis C
Eiger BioPharmaceuticals
 July 2009 Phase 1

Chemical Information & Solubility

Molecular Weight 325.84 Formula

C19H20ClN3
CAS No. 442-52-4 SDF --
Smiles C1CCN(C1)CC2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 65 mg/mL ( (199.48 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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In vivo
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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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