Metyrapone

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Metyrapone

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

54-36-4

包装与价格：

包装	价格(元)
10mM (in 1mL H2O)	电议
50mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	226.27
Cas No.	54-36-4
Formula	C₁₄H₁₄N₂O
Solubility	≥13.45 mg/mL in H2O; ≥42.1 mg/mL in DMSO; ≥59.1 mg/mL in EtOH
Chemical Name	2-methyl-1,2-di(pyridin-3-yl)propan-1-one
Canonical SMILES	O=C(C1=CC=CN=C1)C(C)(C)C2=CC=CN=C2
运输条件	蓝冰运输或根据您的需求运输。
一般建议	为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。

资料参考

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 prostaglandinω/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.

试验操作

Cell experiment:[3]
Cell lines	Non-pigmented epithelial (NPE) cells and pigmented epithelial (PE) cells
Reaction Conditions	2 mM metyrapone
Applications	Metyrapone inhibited cytochrome P450-mediated prostaglandin ω/ω-1 hydroxylase activities in NPE and PE cells.
Animal experiment:[4]
Animal models	A 19.3 kg dog
Dosage form	75 mg/kg Intravenous injection
Applications	A single intravenous injection of metyrapone caused a decrease in adrenal venous 17-hydroxycorticosteroids to 10 percent of the initial value within 10 minutes followed by a return to 75 percent within 3 hours.
Note	The technical data provided above is for reference only.
	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.