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编 号:F397749
分子式:C23H30O4
分子量:370.48
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10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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生物活性:
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.

体内研究:
Nomegestrol acetate (50, 100, 200 mg/kg; p.o.; single daily for 28 days) inhibits growth of RL95-2 xenograft tumors in vivo.Nomegestrol acetate (100, 200 mg/kg; p.o.; single daily for 28 days) surpresses the expression of SUFU and Wnt7a in tumor tissues.Nomegestrol acetate (1, 2.5 mg/rat; p.o.; single daily for 4 days) inhibits ovulation in rats.Animal Model:Female athymic nude mice (BALB/c; 18-20 g; 6 to 7-week-old; xenograft nude mouse model).
Dosage:50, 100, 200 mg/kg
Administration:Oral gavage; single daily for 28 days
Result:Reduced the growth of RL95-2 xenograft tumors in vivo.Upregulated the expression of SUFU and Wnt7a in a dose-dependent manner when at 100 and 200 mg/kg.
Animal Model:Mature female Wistar rats (~200 g).
Dosage:1, 2.5 mg/rat
Administration:Oral administration; single daily for 4 days
Result:Showed only one animal ovulated after receiving 1 mg/kg per day, and no animals ovulated after receiving 2.5 mg/rat per day.

体外研究:
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.Nomegestrol acetate (4, 20, 100 μM; 6, 24, 48 h) upregulates protein levels of SUFU and Wnt7a in RL95-2 cells.
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