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CAS No.: 440122-66-7

WAY-200070 Catalog No. CSN20458

Synonyms: WAY-00005

WAY200070 selectively activates ERβ (EC50 = 2 nM) receptor over ERα (EC50 = 155 nM). It shows anti-depressive and anti-anxiolytic activities.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 ERα

EC50:155nM ERβ

EC50:2nM
描述ER (Estrogen Receptor) is the receptor of estrogens. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. ER has two receptor subtypes, ERα and ERβ. ERα and ERβ have different tissue distributions and each receptor has similar or unique roles in estrogen-dependent gene expressions. WAY-200070 is a selective ERβ agonist. The binding affinity (IC₅₀) of WAY-200070 for human ERβ and ERα were 2 nM and 155 nM, respectively, indicating selectivity towards ERβ^[3]. At the concentration of 10 nM, WAY-200070 significantly decreased proliferation in OVCAR3 and OAW-42 cells^[4]. Within 15 min of administration to mice, WAY-200070 (30 mg/kg s.c.) caused the nuclear translocation of striatal ERβ receptors from the cytosol and also increased c-fos activation 4h after administration, suggesting the binding of WAY-200070 to estrogen receptors and activation of downstream events. Administration of WAY-200070 (30 mg/kg s.c.) to mice produced a delayed ~50% increase in dopamine in the striatum and a delayed and transient ~100% increase in 5-HT, reduced immobility time in the mouse tail suspension test, showed anxiolytic-like effects in the four-plate test (increased punished crossings) and stress-induced hyperthermia (attenuation of hyperthermic response)^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2668 mL
- 16.3339 mL
- 32.6678 mL
- 5 mM
- 0.6534 mL
- 3.2668 mL
- 6.5336 mL
- 10 mM
- 0.3267 mL
- 1.6334 mL
- 3.2668 mL

技术信息

CAS号

440122-66-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C13H8BrNO3

运输

蓝冰

分子量

306.11

别名

WAY-00005

溶解度

DMSO	31.0 mg/mL (101.3 mM)

动物实验配方

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靶点	Description	IC50
ERα		EC50:155nM
ERβ		EC50:2nM

WAY-200070 Catalog No. CSN20458

靶点选择性

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