Clemizole hydrochloride

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Cat.No. 5371 - Clemizole hydrochloride | C19H20ClN3. HCl | CAS No. 1163-36-6
Description: TRPC5 blocker; also H1 antagonist
Chemical Name: 1-[(4-Chlorophenyl)methyl]-2-(1-pyrrolidinylmethyl)-1H-benzimidazole hydrochloride
Purity: ≥99% (HPLC)
Citations (3)
Literature (1)

Biological Activity

TRPC5 channel blocker (IC50 values are 1.1, 6.4, 9.1, 11.3 and 26.5 μM for TRPC5, TRPC4, TRPC3, TRPC6 and TRPC7 respectively). Exhibits minimal effect on TRPM3, TRPM8 and TRPV1-4 channels. Also histamine H1 receptor antagonist and anticonvulsant in zebrafish Dravet syndrome model.

Technical Data

M. Wt 362.3
Formula C19H20ClN3. HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 1163-36-6
PubChem ID 14412
Smiles ClC(C=C4)=CC=C4CN2C(CN3CCCC3)=NC1=CC=CC=C12.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
water 7.25 20
DMSO 18.11 50

Preparing Stock Solutions

The following data is based on the product molecular weight 362.3. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 5.52 mL 27.6 mL 55.2 mL
2.5 mM 1.1 mL 5.52 mL 11.04 mL
5 mM 0.55 mL 2.76 mL 5.52 mL
25 mM 0.11 mL 0.55 mL 1.1 mL

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References are publications that support the biological activity of the product.

Aguilar et al (1986) Pharmacological investigation into the effects of histamine and histamine analogues on guinea-pig and rat colon in vitro. Br.J.Pharmacol. 88 501 PMID: 3742147

Richter et al (2014) Clemizole hydrochloride is a novel and potent inhibitor of transient receptor potential channel TRPC5. Mol.Pharm. 86 514 PMID: 25140002

Baraban et al (2013) Drug screening in Scn1a zebrafish mutant identifies clemizole as a potential Dravet syndrome treatment. Nat.Commun. 4 2410 PMID: 24002024

If you know of a relevant reference for Clemizole hydrochloride, please let us know.

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Keywords: Clemizole hydrochloride, Clemizole hydrochloride supplier, transient, potential, channels, TRPC5, histamine, receptors, blockers, antagonists, TRPC, Histamine, H1, Receptors, 5371, Tocris Bioscience

3 Citations for Clemizole hydrochloride

Citations are publications that use Tocris products. Selected citations for Clemizole hydrochloride include:

Ondrusova et al (2017) Subcutaneous white adipocytes express a light sensitive signaling pathway mediated via a melanopsin/TRPC channel axis. Sci Rep 7 16332 PMID: 29180820

Fernandez-Fernandez et al (2018) Activation of TREK currents by riluzole in three subgroups of cultured mouse nodose ganglion neurons. PLoS One 13 e0199282 PMID: 29928032

Cai and Ford (2018) DA Cells Differentially Regulate Striatal Cholinergic Transmission across Regions through Corelease of DA and Glutamate. Cell Rep 25 3148 PMID: 30540946

Do you know of a great paper that uses Clemizole hydrochloride from Tocris? Please let us know.

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Literature in this Area

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