Metyrapone
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
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.
| 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 |
| SDF | Download SDF |
| 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 | 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。 |
| Cell experiment:[3] | |
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Cell lines |
Non-pigmented epithelial (NPE) cells and pigmented epithelial (PE) cells |
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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] | |
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Animal models |
A 19.3 kg dog |
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Dosage form |
75 mg/kg Intravenous injection |
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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. |
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Note |
The technical data provided above is for reference only. |
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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. |
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质量控制和MSDS
- 批次:
化学结构
