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Megestrol Acetate

商品编号: TL0582
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详细介绍

l  基本信息

产品名称

醋酸甲地孕酮(Megestrol Acetate)

一般描述

Megestrol Acetate(醋酸甲地孕酮) is a synthetic derivative of the naturally occurring female sex hormone progesterone with potential anti-estrogenic and antineoplastic activity.

别 称

17α-Acetoxy-6-methyl-4,6-pregnadiene-3,20-dione; BDH1298, SC10363

纯 度

≥99.0%(HPLC)

CAS NO.

595-33-5

分子式

C24H32O4

分子量

384.516

适用范围

生物试剂,适用于细胞培养等

l  理化信息

外 观

白色或类白色固体

溶解性(25℃)

DMSO

≥30mg/mL

乙醇

≥10mg/mL

Insoluble

l  生物学信息

生物活性/药理作用

Megestrol Acetate is the acetate salt form of megestrol, a synthetic derivative of the naturally occurring female sex hormone progesterone with potential anti-estrogenic and antineoplastic activity. Mimicking the action of progesterone, megestrol acetate binds to and activates nuclear progesterone receptors in the reproductive system, and causes the ligand-receptor complex to be translocated to the nucleus where it binds to and promotes of target genes. This leads to an alteration in protein synthesis, which modulates cell growth of reproductive tissues. Due to the negative feedback mechanism seen with progesterone, megestrol also blocks luteinizing hormone (LH) release from the pituitary gland, thereby leading to an inhibition of ovulation and an alteration in the cervical mucus and endometrium.  Furthermore, without stimulation of LH, estrogen release from the ovaries is stopped, hence impedes the growth of estrogen-sensitive tumor cells.

Primarily hepatic. Megestrol metabolites which were identified in urine constituted 5% to 8% of the dose administered. Respiratory excretion as labeled carbon dioxide and fat storage may have accounted for at least part of the radioactivity not found in urine and feces. No active metabolites have been identified.

The precise mechanism by which megestrol acetate produces effects in anorexia and   cachexia is unknown at the present time, but its progestin antitumour activity may involve suppression of luteinizing hormone by inhibition of pituitary function. Studies also suggest that the megestrol's weight gain effect is related to its appetite-stimulant or metabolic effects rather than its glucocorticoid-like effects or the production of edema. It has also been suggested that megestrol may alter metabolic pathyways via interferences with the production or action of mediators such as cachectin, a hormone that inhibits adipocyte lipogenic enzymes.

l  包装与存储

包 装

1g; 5g

存储温度

0-5

l  注意事项及免责声明

本产品仅用于实验研究,不得作为药物使用,不得用于家用或其它用途。

l  参考文献

1.    http://www.drugbank.ca

2.    https://ncit.nci.nih.gov

3.    https://www.ncbi.nlm.nih.gov