Metyrapone
| 规格 | 价格 | 货期 | 数量 |
|---|---|---|---|
| 1mL(10 mM in H2O) | ¥454.00 | 现货 | |
| 50mg | ¥272.00 | 现货 |
特色产品
- 用于免疫印迹和质谱分析等后续操作
- 适用于30 KDa-130 KDa大小的蛋白
- 可将信号灵敏度提高100倍
- 同时保持稳定的特异性和分辨率
- 提供更高的转录效率并抑制免疫激活
- 使用5-moUTP和Cy5-utp修饰
产品描述
Metyrapone is a cytochrome P450 (CYP) inhibitor. Metyrapone inhibits 11β-hydroxylase (CYP11B1), a key enzyme involved in the final step of cortisol biosynthesis, with an IC50 value of 7.83 μM. Also, metyrapone inhibits other steroidogenic enzymes (e.g. cholesterol side chain cleavage enzyme) at high concentrations. Administration of metyrapone to man and animals (e.g. dogs and sheep) results in a decrease in circulating levels of cortisol. Thus, metyrapone has been used clinically for diagnostic and therapeutic purposes.
References:
1. Sampath-Kumar R, Yu M, Khalil MW, et al. Metyrapone is a competitive inhibitor of 11β-hydroxysteroid dehydrogenase type 1 reductase. The Journal of Steroid Biochemistry and Molecular Biology, 1997, 62(2-3): 195-199.
2. Hays SJ, Tobes MC, Gildersleeve DL, et al. Structure-activity relationship study of the inhibition of adrenal cortical 11β-hydroxylase by new metyrapone analogues. Journal of Medicinal Chemistry, 1984, 27(1): 15-19.
3. Asakura T, Shichi H. Cytochrome P450-mediated prostaglandin ω/ω-1 hydroxylase activities in porcine ciliary body epithelial cells. Experimental Eye Research, 1992, 55(2): 377-384.
4. JENKINS JS, MEAKIN JW, NELSON DH, et al. Inhibition of adrenal steroid 11-oxygenation in the dog. Science, 1958, 128(3322): 478-480.
产品性质
| 物理外观 | A solid |
| CAS号 | 54-36-4 |
| 分子式 | C14H14N2O |
| 分子量 | 226.27 |
| 化学名称 | 2-methyl-1,2-di(pyridin-3-yl)propan-1-one |
| 溶解度 | ≥13.45 mg/mL in H2O; ≥42.1 mg/mL in DMSO; ≥59.1 mg/mL in EtOH |
| SMILES | CC(C)(C(c1cnccc1)=O)c1cnccc1 |
| 存储条件 | -20°C |
| 运输条件 | 蓝冰 |
产品应用 (实验数据来自文献,APExBIO并未验证,仅供参考)
IC50和靶点
| 生物活性描述 | Metyrapone(Su-4885)是一种强效口服活性 11β- 羟化酶抑制剂和自噬激活剂,还能抑制醛固酮的产生。Metyrapone 可抑制内源性肾上腺皮质激素的合成,降低糖皮质激素水平,还可影响行为和情绪。此外,Metyrapone 还可通过下调 mTOR 途径提高自噬过程的效率,并与假单胞菌细胞色素 P-450 相互作用。Metyrapone 可用于研究库欣综合征和抑郁症。 |
| 靶点 | Hydroxylases |



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