aromatase (human)

Exemestane (EXE) is an Aromatase Inhibitor. The mechanism of action of exemestane is as an Aromatase Inhibitor.

Minamestane is a novel irreversible aromatase inhibitor.Minamestane induces time-dependent inhibition of human placental aromatase with a half-life of 4 minutes and a K of 59 nM.Minamestane has antitumor activity.

Prochloraz (Prelude) is a broad-spectrum contact imidazole fungicide. Prochloraz inhibits human placental microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an estrogen receptor (IC50s = 25 μM) and androgen receptor (IC50 = 4 μM) antagonist, and activates aryl hydrocarbon receptors (EC50 = 1 μM).

Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM). Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent.

(S)-Dexfadrostat ((S)-Fadrozole), an aromatase inhibitor, exhibits an IC 50 of 4.6 nM in in vitro assays using human placental microsomes. It is applicable for research on estrogen-dependent breast cancer, gynecomastia, and systemic lupus erythematosus.

YM 511 is a highly specific non-steroidal aromatase inhibitor. YM 511 inhibits aromatase activities in microsomes from rat ovary and human placenta competitively (IC50s of 0.4 and 0.12 nM, respectively). YM 511 slightly inhibits production of other steroid hormones. YM 511 has the potential for suppressing estrogen-dependent action research without affecting serum levels of other steroid hormones.

Obacunone has cytotoxicity in androgen-dependent human prostate Y cells. Obacunone exerts an antivirulence effect on S. Typhimurium and may serve as a lead compound for development of antivirulence strategies for S. Typhimurium. Obacunone may have the pot

17β-hydroxy Exemestane is the primary active metabolite of exemestane . It is formed by metabolism of exemestane by the cytochrome P450 (CYP) isoforms CYP1A and CYP4A11. 17β-hydroxy Exemestane is an aromatase inhibitor (IC50 = 69 nM using human placental microsomes) and an androgen receptor (AR) agonist (IC50 = 39.6 nM) that is selective for AR over estrogen receptor α (ERα; IC50 = 21.2 μM). It stimulates growth of AR- and ERα-positive MCF-7 (EC50 = 2.7 μM) and T47D breast cancer cells (EC50s = 0.43 and 1,500 nM for AR- and ER-mediated growth, respectively) and inhibits proliferation of testosterone-treated aromatase-overexpressing MCF-7aro cells in a concentration-dependent manner. 17β-hydroxy Exemestane (20 mg/kg) inhibits increases in serum cholesterol and LDL levels and prevents decreases in bone mineral density in the lumbar vertebrae and femur, as well as femoral bending strength and compressive strength of the fifth lumbar vertebrae, in ovariectomized rats.

(R)-Fadrozole ((R)-CGS 16949A; FAD286) is a potent nonsteroidal inhibitor. (R)-Fadrozole also inhibits human placental aromatase (pIC 50 = 6.17) and aldosterone biosynthesis. (R)-Fadrozole reverses cardiac fibrosis in spontaneously hypertensive heart failure rats..

Calceolarioside B (Desrhamnosyl isoacteoside) displays inhibition of aromatase. Calceolarioside B displays inhibition of human recombinant PKCalpha.

Fadrozole hydrochloride (CGS 16949A) is a model aromatase inhibitor that effectively suppresses estrogen production in fish ovaries.

10-Chloroestra-1,4-diene-3,17-dione acts as an estrogen receptor α (ERα) agonist, enhancing reporter gene expression in S. cerevisiae with an EC50 of 0.36 nM for the human receptor. Additionally, it functions as an aromatase inhibitor, exhibiting an IC50 of 2.4 µM.

Prochloraz (Standard) is the standard substance of Prochloraz, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Prochloraz (Prelude) is a broad-spectrum contact imidazole fungicide. Prochloraz inhibits human placental microsomal aromatase in vitro (IC50 = 40 nM). Prochloraz also acts as an estrogen receptor (IC50s = 25 μM) and androgen receptor (IC50 = 4 μM) antagonist, and activates aryl hydrocarbon receptors (EC50 = 1 μM).