Mestranol exhibits a high oral antifertility potency in rats, exceeding that of ethynylestradiol at doses greater than 2.0 mg/kg/day, and demonstrates lower oral estrogenic potency than ethynylestradiol at 0.3 mg/kg/day. It shows oral estrogenic activity in uterotropic assays in rats at doses ranging from 100 to 10,000 ng, causing a decrease in weight by 65.3 mg. Mestranol is involved in diverse biological activities, including modulation of Lamin A splicing, mitochondrial fusion, and inhibition of ROR gamma, GCN5L2, and human tyrosyl-DNA phosphodiesterase 1 among others. It also inhibits chronic active B-cell receptor signaling, malarial parasite plastid function, and HP1-beta chromodomain interactions, and corrects the CFTR Delta508 mutation and blocks Ebola virus entry.
In radioligand binding assays, Mestranol shows moderate potency in inhibiting the Norepinephrine Transporter and higher affinity for the Estrogen ERalpha receptor, while displaying weaker interactions with other receptors such as Cannabinoid CB1 and Progesterone receptors. It also exhibits inhibitory effects on the Serotonin transporter and moderate potency against the Sodium Channel, Site 2. Moreover, this compound has shown potent inhibition of the human CYP3A4 enzyme system.
In anti-viral assays, Mestranol demonstrates inhibition of SARS-CoV-2 induced cytotoxicity in Vero E6 and Caco-2 cells, and inhibition of SARS-CoV-2 3CL-Pro protease activity. It also exhibits antifungal activity against Candida albicans and some antibacterial activities against various bacterial strains including Klebsiella pneumoniae and Pseudomonas aeruginosa. Additionally, it shows antiproliferative activity against human MCF7 cells with an IC50 value of 40.0 nM.
In FDA HLAED assays, it shows varied liver enzyme activity, indicating potential effects on liver function. Mestranol also participates in numerous physiological processes as suggested by bioactivity in assays related to liver and kidney functions, electrolyte balance, and hematologic parameters. Overall, Mestranol presents a broad spectrum of bioactivities, making it a significant candidate for further biomedical research across multiple therapeutic areas..
Note: Summary generated by AI. Data source: ChEMBL 