WAY-214156

WAY-214156 is a synthetic nonsteroidal estrogen that acts as a highly selective agonist of the ERβ.[1][2] It is 100-fold selective for the ERβ over the ERα with an IC50 of 4.2 nM (compare to estradiol with IC50 values of ~3–4 nM for both the ERα and ERβ).[1] The drug is less selective for the ERβ than is prinaberel (ERB-041, WAY-202041), another selective ERβ agonist, but is more potent in comparison.[1] WAY-214156 may produce anti-inflammatory effects via the ERβ and has been proposed as a potential treatment for inflammatory conditions such as rheumatoid arthritis.[1][3]

WAY-214156
Identifiers
PubChem CID
ChemSpider
Chemical and physical data
FormulaC19H10N2O3
Molar mass314.300 g·mol−1
3D model (JSmol)

See also

References
  1. Cvoro A, Tatomer D, Tee MK, Zogovic T, Harris HA, Leitman DC (2008). "Selective estrogen receptor-beta agonists repress transcription of proinflammatory genes". J. Immunol. 180 (1): 630–6. doi:10.4049/jimmunol.180.1.630. PMID 18097065.
  2. Serock, Michelle; Wells, Amanda; Khalil, Raouf (2008). "Modulators of Vascular Sex Hormone Receptors and their Effects in Estrogen-Deficiency States Associated with Menopause". Recent Patents on Cardiovascular Drug Discovery. 3 (3): 165–186. doi:10.2174/157489008786263970. ISSN 1574-8901.
  3. Roman-Blas JA, Castañeda S, Cutolo M, Herrero-Beaumont G (2010). "Efficacy and safety of a selective estrogen receptor β agonist, ERB-041, in patients with rheumatoid arthritis: a 12-week, randomized, placebo-controlled, phase II study". Arthritis Care Res (Hoboken). 62 (11): 1588–93. doi:10.1002/acr.20275. PMID 20556817.


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