Metyrapone Tartrate

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Metyrapone Tartrate

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:

908-35-0

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。

生物活性

Metyrapone (Su-4885) Tartrate is a potent and orally active11β-hydroxylaseinhibitor and anautophagyactivator, also inhibits the production ofaldosterone. 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 ofmTORpathway, and interacts withPseudomonas putidacytochrome 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].

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].

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

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.