| 货号 | 14994-250mg |
| 描述 | Metyrapone blocks cortisol synthesis by inhibiting steroid 11β-hydroxylase in adrenal cortex (IC50 = 7.8 μM).1 Metyrapone binds with high affinity to cytochrome P(CYP)450 in hepatic microsomes and induces rat hepatic CYP1A1 and CYP3A gene expression.2,3 It is used to assess adrenal insufficiency, to address hypercortisolism characteristic of Cushing’s syndrome, and may be of clinical value in the treatment of depression and in reducing brain damage resulting from hypoxia-ischemia.4,5,6 |
| 别名 | NSC 25265;SU 4885; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Hays, S.J.,Tobes, M.C.,Gildersleeve, D.L., et al. Structure-activity relationship study of the inhibition of adrenal cortical 11β-hydroxylase by new metyrapone analogues. Journal of Medicinal Chemistry 27(1), 15-19 (1984). 2.Harvey, J.L.,Paine, A.J. and Wright, M.C. Disruption of endogenous regulator homeostasis underlies the mechanism of rat CYP1A1 mRNA induction by metyrapone. Biochemistry Journal 331(1), 273-281 (1998). 3.Paine, A.J.,Villa, P. and Hockin, L.J. Evidence that ligand formation is a mechanism underlying the maintenance of cytochrome P-450 in rat liver cell culture. Biochemistry Journal 188(3), 937-939 (1980). 4.Kamenicky, P.,Droumaquet, C.,Salenave, S., et al. Mitotane, metyrapone, and ketoconazole combination therapy as an alternative to rescue adrenalectomy for severe ACTH-dependent cushing’s syndrome. Journal of Clinical Endocrinology and Metabolism 96(9), 2796-2804 (2011). 5.Sigalas, P.D.,Garg, H.,Watson, S., et al. Metyrapone in treatment-resistant depression. Ther.Adv.Psychopharmacol. 2(4), 139-149 (2012). 6.Hellmich, H.L.,Rojo, D.R.,Micci, M.A., et al. Pathway analysis reveals common pro-survival mechanisms of metyrapone and carbenoxolone after traumatic brain injury. PLoS One 8(1), e53230 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 226.3 |
| 分子式 | C14H14N2O |
| CAS号 | 54-36-4 |
| 稳定性 | ≥ 2 years |
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