Megestrol Acetate(BDH1298)

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	595-33-5
规格:	≥98%

包装与价格：

包装	价格(元)
500mg	电议
1g	电议
2g	电议
5g	电议
10g	电议
50g	电议

产品介绍

Megestrol acetate (formerly BDH1298, SC10363; BDH-1298; SC-10363; Megace; Ovaban; Pallace; Maygace; Megestil; Niagestin) is a synthetic progestogen derivative that has been approved for use in the treatment of breast cancer and loss of appetite. Megestrol Acetate shows potent anti-proliferative activity in vitro against various cancer cell lines such as HepG2 cells with an IC50 value of 260μM.

理化性质和储存条件

Molecular Weight (MW)	384.51
Formula	C24H32O4
CAS No.	595-33-5
Storage	-20℃ for 3 years in powder form
Storage	-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)
Other info	Chemical Name: (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 InChi Key: RQZAXGRLVPAYTJ-GQFGMJRRSA-N InChi Code: InChI=1S/C24H32O4/c1-14-12-18-19(22(4)9-6-17(27)13-21(14)22)7-10-23(5)20(18)8-11-24(23,15(2)25)28-16(3)26/h12-13,18-20H,6-11H2,1-5H3/t18-,19+,20+,22-,23+,24+/m1/s1 SMILES Code: CC(O[C@]1(C(C)=O)CC[C@@]2([H])[C@]3([H])C=C(C)C4=CC(CC[C@]4(C)[C@@]3([H])CC[C@]12C)=O)=O
Synonyms	BDH 1298; SC10363; BDH1298; SC 10363; BDH-1298; SC-10363; Megace; Ovaban; Pallace. Maygace; Megestil; Niagestin.

实验参考方法

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.
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	Rats
Formulation & Dosage	50 mg/kg
References	Eur J Pharmacol. 2011 Mar 11;654(3):217-25; Aquat Toxicol. 2014 May;150:66-72.