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Clomethiazole

Catalog No. T14983Cas No. 533-45-9
Alias 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.

Clomethiazole

Clomethiazole

Purity: 99.06%
Catalog No. T14983Alias Distraneurin, Chlormethiazole, 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLECas No. 533-45-9
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.
Pack SizePriceAvailabilityQuantity
100 mg$41In Stock
200 mg$58In Stock
500 mg$96In Stock
1 mL x 10 mM (in DMSO)$45In Stock
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Purity:99.06%
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Product Introduction

Bioactivity
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].
AliasDistraneurin, Chlormethiazole, 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE
Chemical Properties
Molecular Weight161.65
FormulaC6H8ClNS
Cas No.533-45-9
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 240 mg/mL (1484.69 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM6.1862 mL30.9310 mL61.8620 mL309.3102 mL
5 mM1.2372 mL6.1862 mL12.3724 mL61.8620 mL
10 mM0.6186 mL3.0931 mL6.1862 mL30.9310 mL
20 mM0.3093 mL1.5466 mL3.0931 mL15.4655 mL
50 mM0.1237 mL0.6186 mL1.2372 mL6.1862 mL
100 mM0.0619 mL0.3093 mL0.6186 mL3.0931 mL

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