Megestrol acetate 是具有口服活性的、合成孕激素。Megestrol acetate 可作为食欲刺激素，用于消瘦综合征如恶病质的研究。Megestrol acetate 可下调细胞核和细胞质雄激素受体 (androgen receptors) 的活性。Megestrol acetate 可用于HIV的研究并下调自噬分解代谢途径。
| 生物活性 | Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosolandrogen receptorshuman BPH tissue. Megestrol acetate has the potential forHIVstudy and downregulates autophagic catabolic pathway[1][2][3][4][5].
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体外研究
(In Vitro) | Megestrol acetate alone results in an ICKY of 48.7 p,M in the MCF7/ADR cell line[2].
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体内研究
(In Vivo) | Megestrol acetate (100 or 300 mg/kg, Subcutaneously daily over a 7-day period) is able to reduce the weight loss produced by both TNF and by the MAC16 tumour[1].
| Animal Model: | Pure strain female NMRI mice (age 6 to 8 weeks)[1]. | | Dosage: | 100 or 300 mg/kg (50 mg megestrol acetate was suspended in 3 ml of pure corn oil). | | Administration: | Subcutaneously daily over a 7-day period. | | Result: | Produced a highly significant reversal of the TNF-induced decrease in body weight, accompanied by a significant increase in both food and water intake.
Caused an increase in body weight over a 24-hour period to female NMRI mice.
No effect on blood glucose levels in saline controls, concurrent administration of megestrol acetate with TNF caused a significant increase in blood glucose compared with administration of TNF alone.
Caused a dose-related reduction in the loss of host body weight in animals bearing the MAC16 tumour.
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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 : 20 mg/mL(52.01 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.6007 mL | 13.0036 mL | 26.0071 mL | | 5 mM | 0.5201 mL | 2.6007 mL | 5.2014 mL | | 10 mM | 0.2601 mL | 1.3004 mL | 2.6007 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 mg/mL (5.20 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (5.20 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (5.20 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (5.20 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.0 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 mg/mL (5.20 mM); Clear solution
此方案可获得 ≥ 2 mg/mL (5.20 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 20.0 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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