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Submit ReviewMetyrapone is a cytochrome P450 inhibitor. Blocks glucocorticoid synthesis via inhibition of steroid 11-β hydroxylase (CYP11B1) activity (IC50 = 7.83 μM). Also inhibits CYP3A4 and cytochrome P450-mediated ω/ω-1 hydroxylase activity.
Metyrapone is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 226.27 |
公式 | C14H14N2O |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 54-36-4 |
PubChem ID | 4174 |
InChI Key | FJLBFSROUSIWMA-UHFFFAOYSA-N |
Smiles | O=C(C2=CN=CC=C2)C(C)(C)C1=CC=CN=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
water | 2.26 | 10 | |
DMSO | 22.63 | 100 |
以下数据基于产品分子量 226.27。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 4.42 mL | 22.1 mL | 44.19 mL |
5 mM | 0.88 mL | 4.42 mL | 8.84 mL |
10 mM | 0.44 mL | 2.21 mL | 4.42 mL |
50 mM | 0.09 mL | 0.44 mL | 0.88 mL |
参考文献是支持产品生物活性的出版物。
Hays et al (1984) Structure-activity relationship study of the inhibition of adrenal cortical 11β-hydroxylase by new metyr. analogues. J.Med.Chem. 27 15 PMID: 6606707
Asakura and Shichi (1992) Cytochrome P450-mediated prostaglandin omega/omega-1 hydroxylase activities in porcine ciliary body epithelial cells. Exp.Eye Res. 55 377 PMID: 1426070
Park et al (2005) Structural and dynamic basis of broad substrate specificity, catalytic mechanism and inhibition of cytochrome P450 3A4. J.Am.Chem.Soc. 127 13634 PMID: 16190729
If you know of a relevant reference for Metyrapone, please let us know.
关键词: Metyrapone, Metyrapone supplier, steroid, 11-β, 11-beta, hydroxylase, inhibitors, inhibits, Cytochrome, P450, CYP11B1, CYP3A4, omega/ω-1, omega-1, Hydroxylases, 3292, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Metyrapone 的部分引用包括:
Taves et al (2016) Lymphoid organs of neonatal and adult mice preferentially produce active glucocorticoids from metabolites, not precursors. Brain Behav.Immun. 57 271 PMID: 27165988
Rincón-Cortés et al (2015) Enduring good memories of infant trauma: rescue of adult neurobehavioral deficits via amygdala serotonin and corticosterone interaction. Brain Res 112 881 PMID: 25561533
Liu et al (2014) Chronic stress impairs GABAergic control of amygdala through suppressing the tonic GABAA receptor currents. Mol Brain 7 32 PMID: 24758222
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