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WAY-200070

WAY-200070用途

WAY-200070是选择性的雌激素受体激动剂,IC50值为2.3 nM。

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WAY-200070名称

[ CAS 号 ]:
440122-66-7

[ 中文名 ]:
WAY-200070

[ 英文名 ]:
WAY 200070

[英文别名 ]:

7-Bromo-2-(4-hydroxy-phenyl)-benzooxazol-5-ol
5-Benzoxazolol,7-bromo-2-(4-hydroxyphenyl)
7-BROMO-2-(4-HYDROXYPHENYL)-1,3-BENZOXAZOL-5-OL
7-bromo-2-(4-hydroxyphenyl)-5-benzoxazolol
WAY-200070

WAY-200070生物活性

[ 描述 ]:

WAY-200070是选择性的雌激素受体激动剂,IC50值为2.3 nM。

[ 相关类别 ]:

信号通路 >> 其他 >> 雌激素受体/ERR

研究领域 >> 神经疾病

[ 靶点 ]

IC50: 2.3 nM (ERRβ), 155 nM (ERRα)[1]

[体内研究]

施用WAY-200070(30mg/kg sc)引起WT小鼠中ERRβ受体的核转位。施用WAY-200070(30mg/kg sc)使野生型小鼠的纹状体中的多巴胺延迟50％增加。 WAY-200070(30 mg/kg sc)减少小鼠尾悬吊试验中的不动时间,表明具有抗抑郁样作用[1]。在性腺完整的雄性和雌性小鼠中,WAY-200070增加了激动行为,例如下推和激进的梳理,同时使攻击不受影响[2]。用PPT治疗的卵巢切除(ovx)小鼠未能学习社会获得性偏好,而WAY-200070治疗的ovx小鼠对其示范者食用的食物显示出两倍长的偏好[3]。 WAY-200070显示,在强迫游泳试验中,开放场和高架加迷宫中的焦虑样行为明显减少,并且抑郁样行为明显减少[4]。

[动物实验]

大鼠：在卵巢切除术后1周开始，给动物每日一次皮下注射羟丙基β-环糊精[载体;盐水中27％（wt / vol）; DPN（2.0 mg / kg），S-DPN（2.0 mg / kg），R-DPN（2.0 mg / kg），WAY-200070-3（2.0 mg / kg）或PPT（1.0 mg / kg）总体积为0.2 mL。在第4-7天每日治疗注射后3小时，动物进行行为测试[4]。小鼠：将WAY-200070溶于10％乙醇/ 90％miglyol溶液中。 WAY-200070或载体以10mL / kg体重的体积皮下注射。用载体或WAY-200070（30mg / kg sc）注射雄性ERβKO，ERαKO（均在C57BL / 6背景中）和WT C57BL / 6小鼠。 15分钟后，处死动物并解剖纹状体并在液氮中快速冷冻并储存在-70℃下用于随后的测定[1]。

[参考文献]

[1]. Hughes ZA, et al. WAY-200070, a selective agonist of estrogen receptor beta as a potential novel anxiolytic/antidepressant agent. Neuropharmacology. 2008 Jun;54(7):1136-42.

[2]. Clipperton Allen AE, et al. Agonistic behavior in males and females: effects of an estrogen receptor beta agonist in gonadectomized and gonadally intact mice. Psychoneuroendocrinology. 2010 Aug;35(7):1008-22.

[3]. Clipperton AE, et al. Differential effects of estrogen receptor alpha and beta specific agonists on social learning of food preferences in female mice. Neuropsychopharmacology. 2008 Sep;33(10):2362-75.

[4]. Weiser MJ, et al. Estrogen receptor-beta agonist diarylpropionitrile: biological activities of R- and S-enantiomers on behavior and hormonal response to stress. Endocrinology. 2009 Apr;150(4):1817-25.

[相关活性小分子]

WAY-200070物理化学性质

[ 分子式 ]:
C₁₃H₈BrNO₃

[ 分子量 ]:
306.11200

[ 精确质量 ]:
304.96900

[ PSA ]:
66.49000

[ LogP ]:
3.66850

[ 储存条件 ]:
2-8℃

WAY-200070MSDS

详细MSDS(安全技术说明书)

WAY-200070安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301-H319

[ 警示性声明 ]:
P301 + P310-P305 + P351 + P338

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

WAY-200070合成路线

详细合成路线

WAY-200070上下游产品

WAY-200070上游产品

WAY-200070下游产品

WAY-200070文献

Estrogen receptor β represses Akt signaling in breast cancer cells via downregulation of HER2/HER3 and upregulation of PTEN: implications for tamoxifen sensitivity.

Breast Cancer Res. 13(2) , R43, (2011)

The inhibition of estrogen receptor (ER) α action with the ER antagonist tamoxifen is an established treatment in the majority of breast cancers. De novo or acquired resistance to this therapy is comm...

Antidiabetic actions of an estrogen receptor β selective agonist.

Diabetes 62(6) , 2015-25, (2013)

The estrogen receptor β (ERβ) is emerging as an important player in the physiology of the endocrine pancreas. We evaluated the role and antidiabetic actions of the ERβ selective agonist WAY200070 as a...

Effects of an estrogen receptor alpha agonist on agonistic behaviour in intact and gonadectomized male and female mice.

Psychoneuroendocrinology 36(7) , 981-95, (2011)

Gonadal hormones mediate both affiliative and agonistic social interactions. Research in estrogen receptor alpha (ERα) or beta (ERβ) knockout (KO) mice suggests that ERα increases and ERβ decreases ma...

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