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Cat. No. Name Size Price Add Cart
KI3735Clemizole10 mg$170

Chemical Characteristic

Product NameClemizole
CAS No.442-52-4
Molecular Weight 325.84
FormulaC19H20ClN3
Smilesc1(nc2c(n1Cc1ccc(cc1)Cl)cccc2)CN1CCCC1
Chemical Structure

Biological activities

Clemizole efficiently blocks TRPC5 currents and Ca2+ entry in the low micromolar range (IC50 = 1.0 - 1.3 ?M), as determined by fluorometric [Ca2+]i [1]measurements and patch clamp recordings. Clemizole blocks TRPC5 currents irrespectively of the activation mode, e.g. stimulation of GPCR, hypoosmotic buffer conditions or by the direct activator riluzole. Electrophysiological whole cell recordings revealed that the block was mostly reversible. In vitro, it can be used by 50 ?M in U-87 cells [2]. In vivo, it can be used by 40-120 mg/day in adults [3].

References

[1] Vlahakis JZ, Vukomanovic D, Nakatsu K, et al. Selective inhibition of heme oxygenase-2 activity by analogs of 1-(4-chlorobenzyl)-2-(pyrrolidin-1-ylmethyl)-1H-benzimidazole (clemizole): Exploration of the effects of substituents at the N-1 position. Bioorg Med Chem. 2013,21(21):6788-6795.
[2] Baraban SC, Dinday MT, Hortopan GA. Drug screening in Scn1a zebrafish mutant identifies clemizole as a potential Dravet syndrome treatment. Nat Commun. 2013,4:2410. [3] Richter JM, Schaefer M, Hill K, et al. Clemizole Hydrochloride is a Novel and Potent Inhibitor of Transient Receptor Potential Channel TRPC5. Mol Pharmacol. 2014, 86(5):514-521

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

Our products are used for research, laboratory and further evaluation purposes. They are not for human use.
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