Clomethiazole

SKU: orb1308439

Description

Clomethiazole (Distraneurin) is an orally active anticonvulsant and GABAA receptor agonist, researched for potential use in status epilepticus. It is also employed in vitro as a selective inhibitor of human cytochrome P450 isoforms CYP2A6 and CYP2E1 in metabolic studies.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	533-45-9
MW	161.65
Purity	99.06%
Formula	C₆H₈ClNS
SMILES	Cl.CC1=C(CCCl)SC=N1
Target	Cytochromes P450,GABA Receptor
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (30.93 mM);DMSO:240 mg/mL (1484.69 mM)

Bioactivity

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Target 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. Clomethiazole (1 mM), in the absence of GABA, to α1/β1/γ2 or α1/β2/γ2 subunit-containing cells produced large whole-cell currents. Clomethiazole activate GABAA currents in α1/β1/γ2- and α1/β2/γ2-containing cells ( EC50: 0.3 and 1.5 mM) . 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.

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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insomnia, Inhibitor, GABAReceptor, GABAA, GABA Receptor, Gamma-aminobutyric acid Receptor, inhibit, neuroprotective, anticonvulsant, alcoholism, 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE, CYP2E1, CYP2A6, CYPs, Cytochrome P450, Distraneurin, Clomethiazole, Chlormethiazole, sedative, γ-Aminobutyric acid Receptor

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Compound Identifiers

PubChem CID

19035073 ↗

Key Properties

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No computed properties available.

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Clomethiazole (orb1308439)

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Purity:	99.93%
CAS Number:	6001-74-7
MW:	198.11
Formula:	C₆H₉Cl₂NS

Purity:	>98% (HPLC)
CAS Number:	533-45-9
MW:	161.7
Formula:	C₆H₈ClNS

Clomethiazole

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

Chlormethiazole hydrochloride [orb1309837]

Clomethiazole [orb1217917]

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Clomethiazole (orb1308439)

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