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product name Megestrol Acetate


Description: Megestrol acetate (also known as BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite. Megestrol Acetate could cause minor reduction of tumor size and prolonged survival time in Hepatocellular carcinoma (HCC). In addition, Megestrol Acetate has shown a dose-dependent inhibition on growth of the human liver tumor cells in the HepG2 cell lines with the IC50 value of 260μM in vitro. Furthermore, Megestrol Acetate has also shown a significant suppression of tumor growth. 

References: Eur J Pharmacol. 2011 Mar 11;654(3):217-25; Aquat Toxicol. 2014 May;150:66-72. 



Molecular Weight (MW)

384.51
Formula

C24H32O4 
CAS No.

595-33-5
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 33 mg/mL (85.8 mM)
Water: <1 mg/mL
Ethanol: 15 mg/mL (39.0 mM)
Solubility (In vivo)

 
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/1939499

In Vitro

In vitro activity: Megestrol acetate inhibits the expression of cytoplasmic aromatase through nuclear C/EBPβ in reperfusion injury-induced ischemic rat hippocampus. 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.


Kinase Assay


Cell Assay

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. 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. 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.
Animal model  
Formulation & Dosage  
References Eur J Pharmacol. 2011 Mar 11;654(3):217-25; Aquat Toxicol. 2014 May;150:66-72. 

CX-4945

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Author: Sodium channel

Share this post on:

product name Megestrol Acetate


Description: Megestrol acetate (also known as BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite. Megestrol Acetate could cause minor reduction of tumor size and prolonged survival time in Hepatocellular carcinoma (HCC). In addition, Megestrol Acetate has shown a dose-dependent inhibition on growth of the human liver tumor cells in the HepG2 cell lines with the IC50 value of 260μM in vitro. Furthermore, Megestrol Acetate has also shown a significant suppression of tumor growth. 

References: Eur J Pharmacol. 2011 Mar 11;654(3):217-25; Aquat Toxicol. 2014 May;150:66-72. 



Molecular Weight (MW)

384.51
Formula

C24H32O4 
CAS No.

595-33-5
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 33 mg/mL (85.8 mM)
Water: <1 mg/mL
Ethanol: 15 mg/mL (39.0 mM)
Solubility (In vivo)

 
Synonyms

 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/1939499

In Vitro

In vitro activity: Megestrol acetate inhibits the expression of cytoplasmic aromatase through nuclear C/EBPβ in reperfusion injury-induced ischemic rat hippocampus. 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.


Kinase Assay


Cell Assay

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. 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. 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.
Animal model  
Formulation & Dosage  
References Eur J Pharmacol. 2011 Mar 11;654(3):217-25; Aquat Toxicol. 2014 May;150:66-72. 

CX-4945

Share this post on:

Author: Sodium channel