醋酸孕甾酮, 孕酮受体激动剂

Progesterone receptor Selective Inhibitors | Agonists | Antagonists | Chemicals | Modulators

3篇引用文献

10mM in DMSO

CAS编号: 595-33-5(DMSO)
分子式: C₂₄H₃₂O₄
分子量: 384.51

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库存信息

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货号 (SKU)	包装规格	是否现货	价格	数量
M408438-1ml	1ml	现货

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Compound libraries (12332)

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基本描述

英文别名	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
规格或纯度	10mM in DMSO
英文名称	Megestrol Acetate
生化机理	醋酸甲地孕酮（BDH1298，SC10363）是一种合成孕激素，用于治疗乳腺癌和食欲不振。
储存温度	-80℃储存
运输条件	超低温冰袋运输
作用类型	激动剂
作用机制	孕酮受体激动剂
产品介绍	Megestrol Acetate是一种人工合成的孕酮，抑制HegG2，IC50为260μM。 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%

产品属性

ALogP	3.505
hba_count	4
Rotatable Bond	3

关联靶点（人）

NR3C1 Tclin 糖皮质激素受体(Glucocorticoid receptor) (2 活性数据)

点击查看靶蛋白信息： NR3C1

活性类型	活性值-log(M)	作用机制	期刊	参考文献(PubMed IDs)

名称和识别符

分子类型	小分子
Canonical SMILES	CC(=O)OC1(CCC2C3C=C(C)C4=CC(=O)CCC4(C)C3CCC12C)C(C)=O
分子量	384.51
Reaxy-Rn	3489305
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=3489305&ln=

化学和物理性质

溶解性	Solubility (25°C) In vitro
DMSO(mg / mL) Max Solubility	33
DMSO(mM) Max Solubility	85.82
Water(mg / mL) Max Solubility	<1

安全和危险性（GHS）

Reaxy-Rn	3489305
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=3489305&ln=

SDS英文版

技术规格说明书

Concentration(Compounding value)	9.0-11(mmol/L)
Record the entire process by video	Conform

技术规格说明书

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此产品的引用文献

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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, 98 (195). [PMID:28683411] [10.1016/j.bios.2017.06.056]

参考文献

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, 98 (195). [PMID:28683411] [10.1016/j.bios.2017.06.056]