WAY 200070

Names

[ Name ]:
WAY 200070

[Synonym ]:
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)-1,3-benzoxazol-5-ol 7-bromo-2-(4-hydroxyphenyl)-5-benzoxazolol
7-bromo-2-(4-hydroxyphenyl)-5-benzoxazolol
WAY-200070

Biological Activity

[Description]:

WAY-200070 is a selective estrogen receptor β (ERRβ) agonist with an IC50 of 2.3 nM.

[Related Catalog]:

Signaling Pathways >> Others >> Estrogen Receptor/ERR

Research Areas >> Neurological Disease

[Target]

IC50: 2.3 nM (ERRβ), 155 nM (ERRα)[1]

[In Vivo]

Administration of WAY-200070 (30 mg/kg s.c.) causes nuclear translocation of ERRβ receptors in WT mice. Administration of WAY-200070 (30 mg/kg s.c.) produces a delayed 50% increase in dopamine in the striatum of wild type mice. WAY-200070 (30 mg/kg s.c.) reduces immobility time in the mouse tail suspension test indicating an antidepressant-like effect[1]. In gonadally intact male and female mice WAY-200070 increases agonistic behaviors such as pushing down and aggressive grooming, while leaving attacks unaffected[2]. Ovariectomized (ovx) mice treated with PPT fail to learn the socially acquired preference, while WAY-200070-treated ovx mice shows a two-fold prolonged preference for the food eaten by their demonstrator[3]. WAY-200070, shows significantly decreased anxiety-like behaviors in both the open-field and elevated plus maze and significantly less depressive-like behaviors in the forced swim test[4].

[Animal admin]

Rats: Beginning 1 wk after ovariectomy, animals are given a single daily sc injection of hydroxypropyl betacyclodextran [vehicle; 27% (wt/vol) in saline; DPN (2.0 mg/kg), S-DPN (2.0 mg/kg), R-DPN (2.0 mg/kg), WAY-200070-3 (2.0 mg/kg), or PPT (1.0 mg/kg) in a total volume of 0.2 mL. Three hours after the daily treatment injection on d 4-7, animals undergo behavioral testing[4]. Mice: WAY-200070 is dissolved in a 10% ethanol/90% miglyol solution. WAY-200070 or vehicle is injected subcutaneously at a volume of 10 mL/kg body weight. Male ERβKO, ERαKO (both in C57BL/6 background) and WT C57BL/6 mice are injected with vehicle or WAY-200070 (30 mg/kg s.c.). After 15 min, the animals are sacrificed and the striatum is dissected and quickly frozen in liquid nitrogen and stored at -70°C for subsequent assay[1].

[References]

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₃H₈BrNO₃

[ Molecular Weight ]:
306.11200

[ Exact Mass ]:
304.96900

[ PSA ]:
66.49000

[ LogP ]:
3.66850

[ Storage condition ]:
2-8℃

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H319

[ Precautionary Statements ]:
P301 + P310-P305 + P351 + P338

[ RIDADR ]:
UN 2811 6.1 / PGIII

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

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...