An important group of hormones essential for normal women's maturation and the healthy functioning of reproductive and other tissues. During the reproductive years in women estrogens are primarily made in the ovaries. Estrogen is also normally made in children, men and menopausal women by conversion of androgens in fat and muscle tissues. There are three kinds of estrogens. Estradiol is the ovarian hormone of the premenopausal years, estrone is the hormone of the menopausal years and estriol, a weak estrogen is present in high levels during pregnancy. High levels are associated with nausea, breast tenderness, insulin resistance and fluid retention. OR the name for a family of hormones including estradiol, estrone and estriol.
ONC1-0013B inhibits AR activity in vitro. A. ONC1-0013B structure. B. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 1 day. PSA expression plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). Ki values: ± (ONC1-13B), ± (MDV3100), (ARN-509). Mean±SEM from 5 replicate experiments (except ARN-509). C. LnCAP cells cultured (10% CSS) for 3 days, then treated with tested compounds in presence of 1nM DHT for 5 days. Viable cells plotted as percentage of vehicle control (DMSO; n=2, mean±SEM). IC50 values: 30nM (ONC1-13B), 148nM (MDV3100), 240nM (ARN-509). D. Competitive-binding assay vs AR ligand Fluormone™ (PolarScreen™ Androgen Receptor Competitor Assay). IC50 values: 19nM (DHT), (ONC1-13B), (MDV3100).
In the Oxford Journal of Gerontology Series A: Biological Sciences and Medical Sciences, the popular nonsteroidal SARM LGD 4033 (Ligandrol) has been recently studied for it’s effectiveness and safety in healthy young men. Results were favorable indicated by hormone and lipid levels returning to normal without the use of a post cycle therapy. No dangers were detected throughout the study. although there was noticeable suppression in testosterone and HDL cholesterol, it was not significant enough to cause adverse reactions. Because LGD 4033 is considered one of the strongest and most potent nonsteroidal SARMs available, it is not likely that less potent SARMs will produce any harmful effects (Bhasin, 2010).