Home Neuronal Signaling TRP Channel inhibitor Clemizole

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Clemizole TRP Channel inhibitor

Cat.No.S6410

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 TRP Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 325.84

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 65 mg/mL (199.48 mM)
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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 325.84 Formula

C19H20ClN3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 442-52-4 -- Storage of Stock Solutions

Synonyms N/A Smiles C1CCN(C1)CC2=NC3=CC=CC=C3N2CC4=CC=C(C=C4)Cl

Mechanism of Action

Targets/IC50/Ki
H1 receptor
TRPC5
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, this compound 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 concentrations of this chemical. It 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.
In vivo

This compound 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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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