LY88074 analog 1, a benzothiophene compound with nitrogen-containing non-basic side chains, can be utilized either independently or alongside estrogen or progestin. This agent is effective for mitigating post-menopausal symptoms, including osteoporosis, cardiovascular-related pathological conditions, and estrogen-dependent cancer.
Norgestomet is a steroidal progestin of the 19-norprogesterone group used in veterinary medicine to control estrus and ovulation in cattle. In addition to the progesterone receptor, norgestomet possesses a weak (micromolar) affinity for the glucocorticoid
Demegestone is a progestin, or a synthetic progestogen, and hence is a progesterone receptor agonist, the biological target of progestogens like progesterone. It has no androgenic activity. Previously used to treat luteal insufficiency.
Oxendolone is a steroidal progestin and antiandrogen. Oxendolone binds to the progesterone receptor (Ki = 20 nM) and androgen receptor (AR) (Ki = 320 nM) and acts as a weak but clinically relevant inhibitor of 5α-reductase.
Retroprogesterone, a progestin, may be used for menstrual irregularities in adolescence, for the maintenance of threatened pregnancy, and possibly as an ovulation stimulant.
5α-dihydro Levonorgestrel is a metabolite of the synthetic progestin levonorgestrel . It lacks in vitro and in vivo estrogenic activity, but induces copulatory behavior in male rats when administered at a dose of 1 mg per animal per day.
TH5427 hydrochloride is a potent and selective inhibitor of NUDT5 with an IC50 of 29 nM. It demonstrates a remarkable 690-fold selectivity towards NUDT5 compared to MTH1. Moreover, TH5427 hydrochloride effectively inhibits progestin-dependent, PAR-derived nuclear ATP synthesis in breast cancer cells, thereby impeding chromatin remodeling, gene regulation, and ultimately suppressing proliferation.