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Metabolism GR Megestrol acetate

Megestrol acetate

Catalog No. T1284   CAS 595-33-5
Synonyms: BDH1298, SC10363
Purity 99.72% Datasheet

Megestrol acetate is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.

Megestrol acetate, CAS 595-33-5
Pack Size Availability Price/USD Quantity
5 mg In stock 16.00
10 mg In stock 20.00
25 mg In stock 26.00
50 mg In stock 33.00
100 mg In stock 40.00
200 mg In stock 50.00
500 mg In stock 60.00
1 g In stock 75.00
1 mL * 10 mM (in DMSO) In stock 54.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Megestrol acetate is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.
Targets&IC50 ER,   Glucocorticoid Receptor,  
In vivo Megestrol acetate significantly decreases the circulating concentrations of estradiol (E2) and testosterone (T) in female fish or 11-ketotestosterone (11-KT) in male fish. Megestrol acetate exposure significantly downregulates the transcription of certain genes along the hypothalamic-pituitary-gonadal (HPG) axis. [3] Megestrol acetate produces a progressive deterioration in glucose tolerance, with a significant increase in mean fasting plasma glucose concentrations and decrease in mean plasma glucose clearance rates after 6 months and 12 months of treatment in cats. Megestrol acetate also produces a progressive decrease in both resting plasma cortisol concentrations and cortisol concentrations after ACTH stimulation in cats. [4] Megestrol acetate (50 mg/kg/day) for 9 days significantly increases food and water intake compared with untreated controls. Megestrol acetate (50 mg/kg/day) significantly (90-140%) increases in neuropeptide Y concentrations in the arcuate nucleus (where neuropeptide Y is synthesized), in the lateral hypothalamic area (through which arcuate neurones project) and in the medial preoptic area, ventromedial nucleus and dorsomedial nucleus in rats. [5]

Description

Megestrol acetate is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.

Targets&IC50

ER

Glucocorticoid Receptor

In Vitro

Megestrol acetate inhibits the expression of cytoplasmic aromatase through nuclear C/EBPβ in reperfusion injury-induced ischemic rat hippocampus. [1] Megestrol acetate significantly increases the proliferation, migration, and adipogenic differentiation of adipose-derived stem cells (ASCs) in a dose-dependent manner. Megestrol acetate also upregulates genes downstream of glucocorticoid receptor (GR) in ASCs. [2]

In Vivo

Megestrol acetate significantly decreases the circulating concentrations of estradiol (E2) and testosterone (T) in female fish or 11-ketotestosterone (11-KT) in male fish. Megestrol acetate exposure significantly downregulates the transcription of certain genes along the hypothalamic-pituitary-gonadal (HPG) axis. [3] Megestrol acetate produces a progressive deterioration in glucose tolerance, with a significant increase in mean fasting plasma glucose concentrations and decrease in mean plasma glucose clearance rates after 6 months and 12 months of treatment in cats. Megestrol acetate also produces a progressive decrease in both resting plasma cortisol concentrations and cortisol concentrations after ACTH stimulation in cats. [4] Megestrol acetate (50 mg/kg/day) for 9 days significantly increases food and water intake compared with untreated controls. Megestrol acetate (50 mg/kg/day) significantly (90-140%) increases in neuropeptide Y concentrations in the arcuate nucleus (where neuropeptide Y is synthesized), in the lateral hypothalamic area (through which arcuate neurones project) and in the medial preoptic area, ventromedial nucleus and dorsomedial nucleus in rats. [5]

Synonyms BDH1298, SC10363
Purity 99.72%
Appearance solid
Molecular Weight 384.51
Formula C24H32O4
CAS No. 595-33-5

Storage

-20℃ 3 years powder

-80℃ 2 years in solvent

Solubility Information

DMSO: 19.2 mg/mL (50 mM)

Ethanol: 7.7 mg/mL (20 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Kelicen Ugur P, et al. Eur J Pharmacol, 2011, 654(3), 217-225. 2. Sung JH, et al. Stem Cells Transl Med. 2015 Jul;4(7):789-99. 3. Han J, et al. Aquat Toxicol,2014, 150, 66-72. 4. Peterson ME, et al. Res Vet Sci,1987, 42(3), 354-357. 5. McCarthy HD, et al. Eur J Pharmacol,1994, 265(1-2), 99-102.

Related Compound Libraries

This product is contained In the following compound libraries:
Approved Drug Library Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Anti-infection Compound Library Autophagy Compound Library Endocrinology-Hormones Library FDA-approved Drug Library GPCR Compound Library Anti-cancer Approved drug Library Anti-Metabolism Disease Compound Library

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