Aminoglutethimide

Aminoglutethimide is an aromatase inhibitor with IC50 of 10 μM. Target: Aromatase Aminoglutethimide inhibits ACTH receptor (ACTH-R) mRNA expression in ovine adrenocortical cells in a time-dependent fashion. Aminoglutethimide significantly suppresses steroid secretion and the baseline ACTH-R mRNA expression in a dose-dependent fashion (300 μM AG, 5±1%; 30 μM AG, 64±1%; 3 μM AG, 108±19% compared with control cells, 100±11%) by affecting the gene expression or by decreasing transcript accumulation via an effect on RNA stability, in the human NCI-h295 adrenocortical carcinoma cell line, which expresses functional ACTH receptors and produces steroids of the glucocorticoid, mineralocorticoid and androgen pathway [1, 2]. Aminoglutethimide (150 mg/kg) abolishes the induction of ornithine decarboxylase (ODC) and almost depletes the gonads and plasma of progesterone or testosterone elicited by human chorionic gonadotropin (hCG) in the ovary of adult female mice and the testis of immature male mice, which is related to an inhibition of cAMP-dependent protein kinase (IC50 287 μM) rather than blockade of the steroidogenic pathway [3].

125-84-8

DL-Aminoglutethimide

12352005

H302, H315, H319, H335

Cytochrome P450

Reference compound

Metabolic Enzyme/Protease

Endocrinology

https://www.medchemexpress.com/aminoglutethimide.html

10mM

98.79

DMSO : 50 mg/mL (ultrasonic)

O=C(C(CC)(C1=CC=C(N)C=C1)CC2)NC2=O

C13H16N2O2

232.28

H302, H315, H319, H335

[1]Fassnacht, M., et al., Aminoglutethimide suppresses adrenocorticotropin receptor expression in the NCI-h295 adrenocortical tumor cell line. J Endocrinol, 1998. 159 (1) : p. 35-42.|[2]Neves, M.A., et al., An efficient steroid pharmacophore-based strategy to identify new aromatase inhibitors. Eur J Med Chem, 2009. 44 (10) : p. 4121-7.|[3]Bastida, C.M., et al., Aminoglutethimide, a steroidogenesis inhibitor, abolishes hormonal induction of ornithine decarboxylase in steroidogenic tissues: evidence for its role as cAMP-dependent protein kinase inhibitor. Biochem Biophys Res Commun, 2001. 281 (1) : p. 244-8.

Room Temperature

-20°C, 3 years; 4°C, 2 years (Powder)

Reference compound1

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