Megestrol acetate

SKU: orb1309127

Description

Megestrol acetate is a synthetic progestogen with anti-androgenic properties, used in research for breast and endometrial cancers. It is also applied in studies of cancer-related anorexia and cachexia, with investigations conducted in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Infectious Disease & Virology, Metabolism Research, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 595-33-5
• MW: 384.51
• Purity: 99.99% (May vary between batches)
• Formula: C₂₄H₃₂O₄
• SMILES: [H][C@@]12CC[C@](OC(C)=O)(C(C)=O)[C@@]1(C)CC[C@@]1([H])[C@@]2([H])C=C(C)C2=CC(=O)CC[C@]12C
• Target: Autophagy,Progesterone Receptor,Glucocorticoid Receptor,HIV Protease,Estrogen/progestogen Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (2.6 mM);Ethanol:7.7 mg/mL (20.03 mM);DMSO:10 mg/mL (26.01 mM)

Bioactivity

• Target IC50:
  HegG2:260 μM(ec50)
• 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.
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• In Vitro:
  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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ER, Estrogen Receptor, EstrogenReceptor, Glucocorticoid Receptor, GlucocorticoidReceptor, Megestrol, Megestrol acetate, Megestrol Acetate, HIVProtease, HIV Protease, HIV, Human immunodeficiency virus, Inhibitor, NR3C3, inhibit, Anorexia, Autophagy, BDH 1298, BDH1298, BDH-1298, cachexia, BPH, AIDs, ACS, SC10363, SC-10363, SC 10363, syndrome, progestogen Receptor, progestogenReceptor, Progesterone Receptor, ProgesteroneReceptor

Compound Identifiers

PubChem CID

11683