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Clomethiazole

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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

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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 SizePriceUSA WarehouseGlobal WarehouseQuantity
100 mg$41In StockIn Stock
200 mg$58In StockIn Stock
500 mg$96-In Stock
1 mL x 10 mM (in DMSO)$45In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.06%
Appearance:Liquid
Color:Transparent
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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].
SynonymsDistraneurin, Chlormethiazole, 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE
Chemical Properties
Molecular Weight161.65
FormulaC6H8ClNS
Cas No.533-45-9
SmilesCl.CC1=C(CCCl)SC=N1
Relative Density.1.218 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 240 mg/mL (1484.69 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (30.93 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
% DMSO
%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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