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Metyrapone is an inhibitor of the cytochrome P450 (CYP) enzyme 11beta-hydroxylase (IC50 = 7.83 µM), an enzyme involved in the final step of cortisol biosynthesis. It also induces Cyp1a1 and Cyp3a4 expression in rat hepatic microsomes and inhibits the activity of 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) in sheep liver microsomes. Metyrapone (150 mg/kg, s.c.) suppresses hypoxia-ischemia-induced increases in plasma corticosterone levels and seizures in rats. It also reduces ethanol consumption in alcohol high-preferring rats. Formulations containing metyrapone have been used in the diagnosis of adrenal insufficiency and the treatment of Cushing's disease.Formal Name: 2-methyl-1,2-di-3-pyridinyl-1-propanone. CAS Number: 54-36-4. Synonyms: NSC 25265, SU 4885. Molecular Formula: C14H14N2O. Formula Weight: 226.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml, PBS (pH 7.2): 5 mg/ml. lambdamax: 231, 264 nm. SMILES: O=C(C1=CN=CC=C1)C(C)(C)C2=CC=CN=C2. InChi Code: InChI=1S/C14H14N2O/c1-14(2,12-6-4-8-16-10-12)13(17)11-5-3-7-15-9-11/h3-10H,1-2H3. InChi Key: FJLBFSROUSIWMA-UHFFFAOYSA-N.
Keywords:
NSC 25265, SU 4885, 2-methyl-1,2-di-3-pyridinyl-1-propanone
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