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
Clemizole hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
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 |
|---|---|---|---|
| 1 mM | 2.76 mL | 13.8 mL | 27.6 mL |
| 5 mM | 0.55 mL | 2.76 mL | 5.52 mL |
| 10 mM | 0.28 mL | 1.38 mL | 2.76 mL |
| 50 mM | 0.06 mL | 0.28 mL | 0.55 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
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
Keywords: Clemizole hydrochloride, supplier, transient, potential, channels, TRPC5, histamine, receptors, blockers, antagonists, TRPC, Histamine, H1, Receptors, TRPC, Tocris Bioscience
