美雌醇, 雌激素受体α激动剂

Moligand™

10mM in DMSO

CAS编号: 72-33-3(DMSO)
分子式: C₂₁H₂₆O₂
分子量: 310.43

有货

库存信息

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货号 (SKU)	包装规格	是否现货	价格	数量
M409226-1ml	1ml	现货

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Compound libraries (12332)

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基本描述

英文别名	(17α)-3-methoxy-19-norpregna-1,3,5(10)-trien-20-yn-17-ol
规格或纯度	Moligand™, 10mM in DMSO
英文名称	Mestranol
生化机理	Mestranol 是炔雌醇的 3-甲基醚，它是一种强效的雌激素受体激动剂，可用作口服避孕药。
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	雌激素受体α激动剂
产品介绍	美雌醇 Information Mestranol is the 3-methyl ether of ethinyl estradiol, which is a potentestrogen receptoragonist and used as oral contraceptives. In vitro Mestranol is extensively metabolized to hydroxylated products whose bio- logical activity is less well characterized. In vivo Mestranol (0.2 mg/kg) results in an increased percentage of liver occupied by AHF expressing glutathione S-transferase (PGST) in rats. Mestranol administration increases the focal hepatocyte labeling index compared with the control with a trend at the lower dose and a significant difference at the higher dose. Mestranol (0.02 mg/kg and 0.2 mg/kg diet) results in a decrease in the non-focal labeling index compared with that observed for the corresponding concentration of Mestranol alone. Mestranol significantly increases the non-focal hepatic labeling index in uninitiated rats compared with that observed in rats administered the basal diet only. Mestranol (50 mg/100 g b.wt.) has a significant reduction in the apparent number of alpha-2-adrenoceptors in the frontal cortex and nucleus tractus solitarius (NTS) of rat, while apparent numbers of both alpha-1 and alpha-2-adrenoceptors are depressed in the locus coeruleus. Cell Data cell lines： Concentrations： Incubation Time： Powder Purity:≥99%

产品属性

ALogP	5.112
hba_count	1
Rotatable Bond	1

关联靶点（人）

ESR1 Tclin 雌激素受体(Estrogen receptor) (2 活性数据)

点击查看靶蛋白信息： ESR1

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

SLC6A4 Tclin 钠依赖性血清素转运体(Sodium-dependent serotonin transporter) (2 活性数据)

点击查看靶蛋白信息： SLC6A4

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	COC1=CC2=C(C=C1)C3CCC4(C)C(CCC4(O)C#C)C3CC2
分子量	310.43
Reaxy-Rn	8930321
Reaxys-RN link address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8930321&ln=

化学和物理性质

溶解性	Solubility (25°C) In vitro DMSO: 31 mg/mL (199.75 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility	15
DMSO(mM) Max Solubility	48.32
Water(mg / mL) Max Solubility	<1