Megestrol Acetate|595-33-5|(醋酸甲地孕酮)-陌孚医药/Medlife

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Megestrol Acetate (Synonyms: 醋酸甲地孕酮)

目录号: PC10450 纯度: ≥98%

CAS No. :595-33-5

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PC10450-1g	1g	¥675.00	请登录
PC10450-5g	5g	¥1821.00	请登录
PC10450-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥637.00	请登录

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中文名称

Megestrol Acetate

中文别名

醋酸甲地孕酮;6-甲基-17alpha-羟基孕甾-4,6-二烯-3,20-二酮醋酸酯;甲地孕酮醋酸酯;17α-羟基-6-甲基孕甾-4,6-二烯-3,20-二酮17-醋酸酯;17α-乙酰氧基-6-甲基孕甾-4,6-二烯-3,20-二酮;6-甲基孕甾-4,6-二烯-17α-醇-3,20-二酮-17-醋酸酯;妇宁;去氢甲孕酮;醋酸甲地孕酮 GMP;甲地孕酮乙酸酯;* 醋酸甲地孕酮;6-亚甲基醋酸孕酮;L-鸟氨酸甲酯二盐酸盐;Megestrol Acetate 醋酸甲地孕酮;醋酸甲地孕酮 USP标准品;醋酸甲地孕酮标准品;醋酸甲地孕酮,CP2005, USP, BP, EP;醋酸甲地孕酮-D3;乙基磺酰氯;乙酸甲地孕酮标准品;6-甲基-17Α-羟基孕甾-4,6-二烯-3,20-二酮醋酸酯;标准品;醋酸甲羟孕酮杂质G(EP) 标准品;甲地孕酮,17-乙酸酯标准品;甲地孕酮.17-乙酸酯

英文名称

Megestrol Acetate

英文别名

megestrol acetate;Nomegestrol 17-acetate;Nomegestrol Acetate;17-hydroxy-6-methylpregna-4,6-diene-3,20-dione 17-acetate;Megestryl acetate;17Alpha-Acethoxy-6-Methyl-4,6-Pregnadiene-3,20-Dione;[(8R,9S,10R,13S,14S,17R)-17-acetyl-6,10,13-trimethyl-3-oxo-2,8,9,11,12,14,15,16-octahydro-1H-cyclopenta[a]phenanthren-17-yl] acetate;17-(Acetyloxy)-6-methylpregna-4,6-diene-3,20-dione;Megesgtrol Acetate;17α-Acetoxy-6-methyl-4,6-pregnadiene-3,20-dione;ANDARINE;17α-Acethoxy-6-methyl-4,6-pregnadiene-3,20-dione;17α-Hydroxy-6-methyl-4,6-pregnadiene-3,20-dione 17-Acetate;Megestrol 17-Acetate;17alpha-Acetoxy-6-methylpregna-4,6-diene-3,20-dione;17-Hydroxy-6-methylpregna-4,6-diene-3,20-dione acetate;Megace;Megace ES;Niagestin;Ovarid;Ovaban;Megeron;Pallace;Magestin;Ovaban (Veterinary);Megestrol (Acetate);Megestat;BDH 1298;SC10363;SC 10363;17alpha-Acetoxy-6-dehydro-6-methylprogesterone;TJ2M0FR8ES;Megestrol acetate [USAN];17-Acetoxy-6-methylpregn

Cas No.

595-33-5

分子式

C₂₄H₃₂O₄

分子量

384.51

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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 cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.

性状

Solid

体外研究(In Vitro)

Megestrol acetate alone results in an ICKY of 48.7 p,M in the MCF7/ADR cell line.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Pure strain female NMRI mice (age 6 to 8 weeks).
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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. S A Beck, et al. Effect of megestrol acetate on weight loss induced by tumour necrosis factor alpha and a cachexia-inducing tumour (MAC16) in NMRI mice. Br J Cancer. 1990 Sep;62(3):420-4. [Information]

[2]. L Panasci, et al. Sensitization to doxorubicin resistance in breast cancer cell lines by tamoxifen and megestrol acetate. Biochem Pharmacol. 1996 Oct 11;52(7):1097-102. [Information]

[3]. J Geller, et al. Acute therapy with megestrol acetate decreases nuclear and cytosol androgen receptors in human BPH tissue. Prostate. 1982;3(1):11-5. [Information]

[4]. J H von Roenn, et al. Megestrol acetate for treatment of cachexia associated with human immunodeficiency virus (HIV) infection. Ann Intern Med. 1988 Nov 15;109(10):840-1. [Information]

[5]. Vincenzo Musolino, et al. Megestrol acetate improves cardiac function in a model of cancer cachexia-induced cardiomyopathy by autophagic modulation. J Cachexia Sarcopenia Muscle. 2016 Dec;7(5):555-566. [Information]

溶解度数据

体外研究:

DMSO : 20 mg/mL (52.01 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

建议依照次序添加每种溶剂： 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。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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