Bioactivity | Nomegestrol acetate is an orally active, highly selective progestogen and a progesterone receptor complete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrial cancer RL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used in cancer (especially endometrial cancer) and contraceptive studies[1][2][3]. | ||||||||||||
Target | Progesterone receptor. | ||||||||||||
Invitro | Nomegestrol acetate (0.3, 1, 3, 10, 30, 100 µM; 24, 48, 72 h) shows anti-proliferative activity against RL95-2 cells in a dose-dependent manner[1].Nomegestrol acetate (4, 20, 100 µM; 6, 24, 48 h) upregulates protein levels of SUFU and Wnt7a in RL95-2 cells[1]. Cell Proliferation Assay[1] Cell Line: | ||||||||||||
In Vivo | Nomegestrol acetate (50, 100, 200 mg/kg; p.o.; single daily for 28 days) inhibits growth of RL95-2 xenograft tumors in vivo[1].Nomegestrol acetate (100, 200 mg/kg; p.o.; single daily for 28 days) surpresses the expression of SUFU and Wnt7a in tumor tissues[1].Nomegestrol acetate (1, 2.5 mg/rat; p.o.; single daily for 4 days) inhibits ovulation in rats[2]. Animal Model: | ||||||||||||
Name | Nomegestrol acetate | ||||||||||||
CAS | 58652-20-3 | ||||||||||||
Formula | C23H30O4 | ||||||||||||
Molar Mass | 370.48 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Ma AY, et al. Nomegestrol Acetate Suppresses Human Endometrial Cancer RL95-2 Cells Proliferation In Vitro and In Vivo Possibly Related to Upregulating Expression of SUFU and Wnt7a. Int J Mol Sci. 2017 Jun 22;18(7):1337. [2]. van Diepen HA, et al. Nomegestrol acetate: steroid receptor transactivation profile in Chinese hamster ovary cells and ovulation inhibition in rat and monkey. Contraception. 2011 Aug;84(2):199-204. [3]. Mueck AO, et al. Nomegestrol acetate, a novel progestogen for oral contraception. Steroids. 2011 May;76(6):531-9. |