Metyrapone Tartrate (Synonyms: Su-4885 Tartrate)

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物，专注于信号通路和疾病研究领域。
Metyrapone Tartrate  (Synonyms: Su-4885 Tartrate)

Metyrapone (Su-4885) Tartrate 是一种有效且具有口服活性的 11β-羟化酶 (11β-hydroxylase) 抑制剂，可抑制醛固酮 (aldosterone) 的产生，也是一种细胞自噬 (autophagy) 激活剂。Metyrapone Tartrate 能抑制内源性肾上腺皮质激素的合成，也会影响行为和情绪。此外，Metyrapone Tartrate 可通过下调 mTOR 通路增加自噬过程的效率，也能与恶臭假单胞菌 (Pseudomonas putida) 细胞色素 P-450 (CYP450) 相互作用。Metyrapone Tartrate 可用于研究库兴氏综合征 (Cushing’s syndrome) 和抑郁症。

Metyrapone Tartrate (Synonyms: Su-4885 Tartrate)

Metyrapone Tartrate Chemical Structure

CAS No. : 908-35-0

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Metyrapone Tartrate 的其他形式现货产品:

Metyrapone

Metyrapone Tartrate 相关产品

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生物活性

Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone Tartrate can be used for researching Cushing’s syndrome and depression[1][2][3][4][5].

IC50 & Target

11β-hydroxylase, Aldosterone, CYP450, Autophagy[1][4][5]
体外研究
(In Vitro)

Metyrapone (100 μM; 2 h) hyperactivates autophagy in HepG2, and delays the activation of apoptosis at severe endoplasmic reticulum (ER) stress[5].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Metyrapone Tartrate 相关抗体:
体内研究
(In Vivo)

Metyrapone (25 or 50 mg/kg; SC, single dosage) decreases the stress-induced increase in plasma corticosterone levels, significantly impairs acquisition performance at high dosage, and increases open arm activity at low dosage[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley rats (n=179; 270-300g)[1]
Dosage: 25 or 50 mg/kg (in a volume of 2.0 ml/kg)
Administration: SC, single dosage
Result: Dose-dependently decreased the stress-induced increase in plasma corticosterone levels in the water maze test; the high level dose significantly impaired acquisition performance in the water maze and decreased fear-induced immobility; the lower dose increased open arm activity.

Clinical Trial

分子量

526.45

Formula

C22H26N2O13
CAS 号

908-35-0
结构分类
  • Alkaloids
  • Pyridine Alkaloids
初始来源
  • 内源性代谢物
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (544 KB) 产品使用指南 (1538 KB)

参考文献

  • [1]. Roozendaal B, et al. Dose-dependent suppression of adrenocortical activity with metyrapone: effects on emotion and memory. Psychoneuroendocrinology. 1996 Nov;21(8):681-93.  [Content Brief]

    [2]. Jahn H, et al. Metyrapone as additive treatment in major depression: a double-blind and placebo-controlled trial. Arch Gen Psychiatry. 2004 Dec;61(12):1235-44.  [Content Brief]

    [3]. Daniel E, et al. Effectiveness of Metyrapone in Treating Cushing’s Syndrome: A Retrospective Multicenter Study in 195 Patients. J Clin Endocrinol Metab. 2015 Nov;100(11):4146-54.  [Content Brief]

    [4]. Peterson JA, Ullrich V, Hildebrandt AG. Methyrapone interaction with Pseudomonas putida cytochrome P-405. Arch Biochem Biophys. 1971 Aug;145(2):531-42.  [Content Brief]

    [5]. Holczer M, et al. A Comprehensive Systems Biological Study of Autophagy-Apoptosis Crosstalk during Endoplasmic Reticulum Stress. Biomed Res Int. 2015;2015:319589.  [Content Brief]

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