WAY 200070

ERRβ (IC50 = 2.3 nM); ERRα (IC50 = 155 nM)

WAY 200070 is a novel and selective agonist that has antidepressant properties for the estrogen receptor β (ERRβ). With an IC50 of 2.3 nM, it activates ERRβ. In animal models, estrogen has been shown in recent studies to have effects similar to those of antidepressants. WAY-200070, an ERRβ agonist, has been demonstrated in several in vivo mouse models to exhibit anxiolytic and antidepressant properties. WAY-200070 (30 mg/kg s.c.) caused striatal ER beta receptors from the cytosol to move into the nucleus after administration. Moreover, four hours after administration, WAY-200070 raised c-fos activation, but not fifteen minutes later. WAY-200070 has bound to estrogen receptors and triggered downstream events, as evidenced by its nuclear translocation and c-fos induction effects. The fact that these effects are absent in ER beta KO mice indicates that WAY-200070 was specifically targeting ER beta. The striatum of wild type mice showed a delayed, roughly 50% increase in dopamine following the administration of WAY-200070 (30 mg/kg s.c.).

In animal models, estrogen has been shown in recent studies to have effects similar to those of antidepressants. WAY-200070, an ERRβ agonist, has been demonstrated in several in vivo mouse models to exhibit anxiolytic and antidepressant properties. WAY-200070 (30 mg/kg s.c.) caused striatal ER beta receptors from the cytosol to move into the nucleus after administration. Moreover, four hours after administration, WAY-200070 raised c-fos activation, but not fifteen minutes later. WAY-200070 has bound to estrogen receptors and triggered downstream events, as evidenced by its nuclear translocation and c-fos induction effects. The fact that these effects are absent in ER beta KO mice indicates that WAY-200070 was specifically targeting ER beta. The striatum of wild type mice showed a delayed, roughly 50% increase in dopamine following the administration of WAY-200070 (30 mg/kg s.c.). The effect persisted for 90 to 240 minutes and was noteworthy. Mice with ER beta KO did not exhibit this increase. WAY-200070 (30 mg/kg s.c.) also caused a temporary, delayed increase in 5-HT levels in wild type mice by about 100%. 5-HTP accumulation was assessed in order to learn more about the impact of ER beta receptors on serotonergic function. It was discovered that ER beta KO mice had lower frontal cortex 5-HTP levels, which suggests lower tryptophan hydroxylase activity. In behavioral models, WAY-200070 (3–30 mg/kg s.c.) was also tested. In the mouse tail suspension test, WAY-200070 (30 mg/kg s.c.) shortened the immobility duration, suggesting an antidepressant-like effect. In the four-plate test, WAY-200070 (30 mg/kg) demonstrated effects similar to those of anxiolytics (more punished crossings) and stress-induced hyperthermia (attenuation of hyperthermic response). Positive modulation of ER beta function may offer a novel treatment for affective disorders, as supported by the effects of the selective ER beta agonist WAY-200070 on dopamine and serotonin, as well as the genotype-specific effects on neurochemistry and anxiolytic and antidepressant-like effects.

WAY-200070 has a 2.3 nM IC50 and acts as a selective agonist of the estrogen receptor β (ERRβ).

For neurochemistry and in vitro studies, mice with and without ER beta KO were used. Male ERβKO, ERαKO, and wild type C57BL/6 mice (10–12 weeks old; Taconic) were the mice used in the models. The tail suspension test was performed on male Swiss Webster mice (25–35 g, Charles River). The stress-induced hyperthermia and control microdialysis experiments were conducted on male C57Bl/6 mice (25–35 g, Taconic).

[1]. Neuropharmacology . 2008 Jun;54(7):1136-42.

C13H8BRNO3

306.12

304.97

C, 51.01; H, 2.63; Br, 26.10; N, 4.58; O, 15.68

440122-66-7

White to beige solid powder

C1=CC(=CC=C1C2=NC3=C(O2)C(=CC(=C3)O)Br)O

BAAILVWEAXFTSF-UHFFFAOYSA-N

InChI=1S/C13H8BrNO3/c14-10-5-9(17)6-11-12(10)18-13(15-11)7-1-3-8(16)4-2-7/h1-6,16-17H

7-bromo-2-(4-hydroxyphenyl)-1,3-benzoxazol-5-ol

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility in Formulation 1: ≥ 10 mg/mL (32.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 2: ≥ 10 mg/mL (32.67 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 100.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)