Megestrol Acetate - 10mM in DMSO , Progesterone receptor agonist, CAS No.595-33-5, Progesterone receptor agonist

CAS: 595-33-5 Cat. No.: M408438 Molecular Weight: 384.52 Beilstein Registry Number: 8(4)2431 EC Number: 209-864-5

GRADE & PURITY 10mM in DMSO

Synonyms

BDH1298, SC10363 | (8R,9S,10R,13S,14S,17R)-17-acetyl-6,10,13-trimethyl-3-oxo-2,3,8,9,10,11,12,13,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Megestrol acetate (BDH1298, SC10363) is a syntheticprogestogen, used to treat breast cancer and loss of appetite.
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.

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.
Cell Data

cell lines：HCT116, MDA-MB-231, SNU-5, and MKN45 cells

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

BDH1298, SC10363 | (8R, 9S, 10R, 13S, 14S, 17R)-17-acetyl-6, 10, 13-trimethyl-3-oxo-2, 3, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17-dodecahydro-1H-cyclopenta[a]phenanthren-17-yl acetate

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

Megestrol acetate (BDH1298, SC10363) is a synthetic progestogen, used to treat breast cancer and loss of appetite.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

AGONIST

Mechanism of action

Progesterone receptor agonist

Names and Identifiers

• Isomeric SMILES: CC1=C[C@@H]2[C@H](CC[C@]3([C@H]2CC[C@@]3(C(=O)C)OC(=O)C)C)[C@@]4(C1=CC(=O)CC4)C
• RTECS: TU4075000
• Molecular Weight: 384.52
• Beilstein: 8(4)2431
• Reaxy-Rn: 3489305
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=3489305&ln=

Associated Targets(Human)

NR3C1 Tclin Glucocorticoid receptor (2 Activities)

Discover Target: NR3C1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro
• Specific Rotation[α]: 11° (C=2,CHCl3)
• Melt Point(°C): 218 °C

References

1. Zu Qiang Jiang, Lei Zhang, Cui Juan Lan, Jian Ping Wang.  (2023)  Development of a Progesterone-Receptor-Based Pseudo-immunoassay for Multi-detection of Progestins in Milk and Studying Its Recognition Mechanism.  JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY,      [PMID:37938156] [10.1021/acs.jafc.3c05890]

2. Yan Su, Gelin Liu, Haozhe Hou, Yaojia Peng, Jianping Wang.  (2023)  Development of a Magnetic Molecularly Imprinted Microsphere-Based Signal Amplified Semi-Homogeneous Method for Multidetection of Five Progestins in Milk.  Foods,  12  (15): (2818).  [PMID:37569089] [10.3390/foods12152818]

3. Mai Luo, Yifan Hua, Yiran Liang, Jiajun Han, Donghui Liu, Wenting Zhao, Peng Wang.  (2017)  Synthesis of novel β-cyclodextrin functionalized S, N codoped carbon dots for selective detection of testosterone.  BIOSENSORS & BIOELECTRONICS,      [PMID:28683411] [10.1016/j.bios.2017.06.056]

4. Aining Yin, Yu Fu, Tingxin Wang, Honglin Li, Xiufang Wang, Xueke Ye, Peipei Dong, Wei Yao.  (2024)  Fu-Zheng-Li-Fei Recipe (FZLFR) in the treatment of cancer cachexia: Exploration of the efficacy and molecular mechanism based on chemical characterization, experimental research and network pharmacology.  JOURNAL OF ETHNOPHARMACOLOGY,      [PMID:39395766] [10.1016/j.jep.2024.118929]