Dienogest

Dienogest (STS-557) is an orally active and selective progesterone receptor agonist that effectively reduces the gene expression of COX-2, mPGES-1 and aromatase. Dienogest also inhibits the mRNA and protein expression of PGE₂ synthase and the activation of NF-κB. Dienogest can be used in studies of endometriosis, menopause and menorrhagia^[1][2]. In Vitro: Dienogest (0.01-1 µM; 24 h) inhibits PGE₂ production via inhibition of PGE₂ synthase gene expressions with the concomitant inhibition of NF-κB activity in a spheroid culture^[1].
Dienogest (0.1 µM; 24 h) inhibits aromatase expression gene along with COUP-TFII mRNA expression in a PGE₂-independent manner^[1]. In Vivo: Dienogest (1 mg/kg; p.o.; once daily for 14 days) regulates angiogenesis in ectopic endometrial lesions in rat endometrial autograft model^[2].