Nomegestrol acetate 是一种口服有效的高选择性孕激素，也是孕酮受体 (progesterone receptor) 完全激动剂，能抑制排卵。Nomegestrol acetate 还能有效抑制人类子宫内膜癌 RL95-2 细胞体外和体内增殖。Nomegestrol acetate 可用于癌症 (尤其是子宫内膜癌) 和避孕的研究。
| 生物活性 | Nomegestrol acetate is an orally active, highly selective progestogen and aprogesterone receptorcomplete agonist. Nomegestrol acetate inhibits ovulation. Nomegestrol acetate is also effective in inhibiting the proliferation of human endometrialcancerRL95-2 cells in vitro and in vivo. Nomegestrol acetate can be used incancer(especially endometrial cancer) and contraceptive studies[1][2][3]. |
| IC50& Target | Progesterone receptor[3]. |
体外研究
(In Vitro) | 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: | RL95-2 cells | | Concentration: | 0.3, 1, 3, 10, 30, and 100 μM | | Incubation Time: | 24, 48, 72 h | | Result: | Inhibited the growth of RL95-2 cells in a concentration-dependent manner, with IC50values of 19.88, 21.62 and 52.80 μM for 48, 72 and 24 h. |
Western Blot Analysis[1] | Cell Line: | RL95-2 cells | | Concentration: | 4, 20, 100 μM | | Incubation Time: | 6, 24, 48 h | | Result: | Increased the protein levels of SUFU and Wnt7a (relative to GAPDH expression) in a concentration-dependent manner. |
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体内研究
(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: | Female athymic nude mice (BALB/c; 18-20 g; 6 to 7-week-old; xenograft nude mouse model)[1]. | | 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)[2]. | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 62.5 mg/mL(168.70 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6992 mL | 13.4960 mL | 26.9920 mL | | 5 mM | 0.5398 mL | 2.6992 mL | 5.3984 mL | | 10 mM | 0.2699 mL | 1.3496 mL | 2.6992 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (5.61 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.61 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (5.61 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.61 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (5.61 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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