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)
Datasheet
Citations
Reviews
Literature

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.

Compound Libraries

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Technical Data

M. Wt 362.3
Formula C19H20ClN3. HCl
Storage Desiccate at RT
Purity ≥99% (HPLC)
CAS Number 1163-36-6
PubChem ID 14412
InChI Key DNFMJYXRIMLMBZ-UHFFFAOYSA-N
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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

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


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Literature in this Area

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