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Clomethiazole

Catalog No. T14983 CAS 533-45-9

Synonyms: Distraneurin, Chlormethiazole, 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE

Clomethiazole (Distraneurin) is an orally active GABAA agonist and it is an anticonvulsant agent. It also has the potential for treating convulsive status epilepticus. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes.

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Clomethiazole, CAS 533-45-9

Pack Size	Availability	Price/USD
100 mg	In stock	$ 41.00
200 mg	In stock	$ 58.00
500 mg	In stock	$ 96.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 98.43%

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Description	Clomethiazole (Distraneurin) is an orally active GABAA agonist and it is an anticonvulsant agent. It also has the potential for treating convulsive status epilepticus. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes.
Targets&IC50	CYP2A6/CYP2E1:24 µM and 42 µM
In vitro	Clomethiazole inhibits cytochrome P450 isoforms, CYP2A6 and CYP2E1 (IC50: 24 μM and 42 μ), in human liver microsomes. But all other isoforms exhibiting values > 300 μM[2]. Clomethiazole (1 mM), in the absence of GABA, to α1/β1/γ2 or α1/β2/γ2 subunit-containing cells produced large whole-cell currents[1]. Clomethiazole activate GABAA currents in α1/β1/γ2- and α1/β2/γ2-containing cells ( EC50: 0.3 and 1.5 mM) [1]. Clomethiazole (30 μM) at low concentration also potentiates the action of GABA in both cell types, equivalent to a 3-fold increase in potency and up to 1.8-fold increase in maximal current[1].

Synonyms	Distraneurin, Chlormethiazole, 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE
Molecular Weight	161.65
Formula	C6H8ClNS
CAS No.	533-45-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 240 mg/mL (1484.69 mM), Sonication is recommended.

References and Literature

1. Nelson RM, et al.Electrophysiological actions of gamma-aminobutyric acid and clomethiazole on recombinant GABA(A) receptors.Eur J Pharmacol. 2002 Oct 11;452(3):255-62. 2. Stresser DM, et al. Selective Time- and NADPH-Dependent Inhibition of Human CYP2E1 by Clomethiazole.Drug Metab Dispos. 2016 Aug;44(8):1424-30

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library Bioactive Compounds Library Max Metabolism Compound Library Anti-Aging Compound Library Orally Active Compound Library

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Keywords

Clomethiazole 533-45-9 Membrane transporter/Ion channel Metabolism Neuroscience P450 GABA Receptor inhibit Distraneurin Cytochrome P450 sedative anticonvulsant Gamma-aminobutyric acid Receptor Chlormethiazole alcoholism insomnia CYPs Inhibitor neuroprotective γ-Aminobutyric acid Receptor 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE inhibitor

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