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Cat. No. Name Size Price Add Cart
KI0810Aminoglutethimide1 g$250

Chemical Characteristic

Product NameAminoglutethimide
SynonymsCytadren
CAS No.125-84-8
Molecular Weight 232.28
FormulaC13H16N2O2
Chemical Structure

Biological activities

Aminoglutethimide is an aromatase inhibitor with an IC50 of 20 µM.[1] Aminoglutethimide inhibits human placental aromatase activity with an apparent Ki value of 0.7 µM. Aminoglutethimide inhibits the aromatase activity of uterine leiomyoma and cultured choriocarcinoma Enami cells as well as immunopurified human placental aromatase cytochrome P-450 by more than 90%, with IC50 values ranging from 5 to 7 µM. Aminoglutethimide inhibits bovine adrenal cholesterol side-chain cleavage activity with an IC50 value of 40 µM and inhibits 21-hydroxylase activity slightly, but does not inhibit 17α-, 11β- and 18-hydroxylase at concentrations up to 100 µM.[2] Aminoglutethimide is a 10-fold more potent aromatase inhibitor than is testololactone, but is less potent than are 4-hydroxyan-drostenedione and several brominated androstenedione derivatives. In vitro, aminoglutethimide can effectively block aromatase directly in human breast tumors.[3] In vivo administration of aminoglutethimide produces a dose-related increase in activities attributable to the hepatic P450 enzyme 2B1 in rat. Aminoglutethimide administration (25 and 50 mg/kg) results in 85 and 100% increases in testosterone 16 beta-hydroxylation and 3.3- and 7.4-fold increases in 7-pentylresorufin O-depentylation (both mediated by P450 2B1) in rat liver.[4]

Protocols

In vitro: Aminoglutethimide is dissolved in 65% ethanol as a stock solution.[5]

References

[1] Miller WR, et al. Biology of aromatase inhibitors: pharmacology/endocrinology within the breast. Endocr Relat Cancer. 1999, 6(2): 187-195. 閵嗏偓閵嗏偓
[2] Kitawaki J, et al. Selective aromatase inhibition by pyridoglutethimide, an analogue of aminoglutethimide. Acta Endocrinol (Copenh). 1990, 122(5): 592-598. 閵嗏偓閵嗏偓
[3] Santen RJ, et al. In vivo and in vitro pharmacological studies of aminoglutethimide as an aromatase inhibitor. Cancer Res. 1982, 42(8 Suppl): 3353s-3359s. 閵嗏偓閵嗏偓
[4] Murray M, et al. Induction of cytochrome P450 2B1 in rat liver by the aromatase inhibitor aminoglutethimide. J Pharmacol Exp Ther. 1993, 265(1): 477-481. 閵嗏偓閵嗏偓
[5] Fassnacht M, et al. Aminoglutethimide suppresses adrenocorticotropin receptor expression in the NCI-h295 adrenocortical tumor cell line. J Endocrinol. 1998, 159(1): 35-42. 閵嗏偓閵嗏偓

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KareBayTM provides scientists and clinicians with a wide range of biotechnological products and science lab supplies for chemical research and analyzing life processes. KareBay's extensive capabilities include commercializing reagents and kits, manufacturing biotech products and providing contract research services to organizations worldwide. Our many global labs, offices, and business partners enable KareBay to extend its products and services to its customer base around the world.

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