Merck
CN

PZ0183

Sigma-Aldrich

ERB-041

≥98% (HPLC)

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别名:
2-(3-氟-4-羟基苯基)-7-乙烯基-1,3-苯并恶唑-5-醇, WAY-202041, 普林贝瑞
经验公式(希尔记法):
C15H10FNO3
分子量:
271.24
MDL编号:
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to tan

溶解性

DMSO: ≥25 mg/mL

储存温度

room temp

SMILES字符串

OC(C=C1)=C(F)C=C1C2=NC3=CC(O)=CC(C=C)=C3O2

InChI

1S/C15H10FNO3/c1-2-8-5-10(18)7-12-14(8)20-15(17-12)9-3-4-13(19)11(16)6-9/h2-7,18-19H,1H2

InChI key

MQIMZDXIAHJKQP-UHFFFAOYSA-N

基因信息

human ... ESR2(2100)

生化/生理作用

ERB-041 是一种强效、选择性雌激素 ERβ 受体激动剂(IC50 ERβ:5.4 nM;选择性是 ERα 的 200 倍以上)。ERβ 在子宫、下丘脑/垂体、骨骼和其他经典雌激素靶组织中介导雌激素作用的作用较小。然而,目前已经确立 ERβ 在卵巢、心血管系统和脑以及炎症动物模型(包括关节炎、子宫内膜异位症、炎症性肠病和败血症)中的明确作用。人们对寻找 ERβ 激动剂越来越感兴趣,其可用于各种临床应用而不会引发经典的雌激素副作用。

特点和优势

该化合物是受体分类及信号转导手册上核受体(类固醇)页面上的特色化合物。想要浏览手册的其他页面, 请单击此处

象形图

Exclamation mark

警示用语:

Warning

危险声明

危险分类

Acute Tox. 4 Oral - Eye Irrit. 2

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Geriolda Topi et al.
The Journal of pathology, 251(3), 297-309 (2020-04-26)
Oestrogen receptor β (ERβ) has been suggested to have anti-proliferative and anti-tumour effects in breast and prostate cancer cells, but other studies have indicated its tumour-promoting effects. Understanding the complex effects of this receptor in different contexts requires further study.
Sreenivasan Paruthiyil et al.
PloS one, 4(7), e6271-e6271 (2009-07-18)
Estrogens produce biological effects by interacting with two estrogen receptors, ERalpha and ERbeta. Drugs that selectively target ERalpha or ERbeta might be safer for conditions that have been traditionally treated with non-selective estrogens. Several synthetic and natural ERbeta-selective compounds have
Qian Jiang et al.
Purinergic signalling, 13(1), 105-117 (2016-11-07)
Estrogen receptor beta (ERβ) has been shown to play a therapeutic role in inflammatory bowel disease (IBD). However, the mechanism underlying how ERβ exerts therapeutic effects and its relationship with P2X3 receptors (P2X3R) in rats with inflammation is not known.
Iuliia Savchuk et al.
PloS one, 8(8), e71722-e71722 (2013-08-24)
It is well known that estrogens and estrogen-like endocrine disruptors can suppress steroidogenic gene expression, attenuate androgen production and decrease differentiation of adult Leydig cell lineage. However, there is no information about the possible link between the potency of Leydig
Lili Zhang et al.
PloS one, 5(7), e11791-e11791 (2010-07-30)
Estrogens are used extensively to treat hot flashes in menopausal women. Some of the beneficial effects of estrogens in hormone therapy on the brain might be due to nongenomic effects in neurons such as the rapid stimulation of calcium oscillations.

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