Nomegestrol acetate

• CAT Number: R048067
• CAS Number: 58652-20-3
• Molecular Formula: C23H30O4
• Molecular Weight: 370.48
• Purity: ≥95%
• Synonyms: [(8S,9S,10R,13S,14S,17R)-17-acetyl-6,13-dimethyl-3-oxo-1,2,8,9,10,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-17-yl] acetate
• InChI: InChI=1S/C23H30O4/c1-13-11-20-18(17-6-5-16(26)12-19(13)17)7-9-22(4)21(20)8-10-23(22,14(2)24)27-15(3)25/h11-12,17-18,20-21H,5-10H2,1-4H3/t17-,18-,20-,21+,22+,23+/m1/s1
• InChIKey: IIVBFTNIGYRNQY-YQLZSBIMSA-N
• SMILES: CC1=CC2C(CCC3(C2CCC3(C(=O)C)OC(=O)C)C)C4C1=CC(=O)CC4

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].
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].
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].

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.
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[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.
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[3]. Mueck AO, et al. Nomegestrol acetate, a novel progestogen for oral contraception. Steroids. 2011 May;76(6):531-9.
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