Chemistry:WAY-214156
From HandWiki
Short description: Chemical compound
 | |
| Identifiers | |
|---|---|
| |
| PubChem CID | |
| ChemSpider | |
| Chemical and physical data | |
| Formula | C19H10N2O3 |
| Molar mass | 314.300 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
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]
See also
References
- ↑ 1.0 1.1 1.2 1.3 "Selective estrogen receptor-beta agonists repress transcription of proinflammatory genes". Journal of Immunology 180 (1): 630–636. January 2008. doi:10.4049/jimmunol.180.1.630. PMID 18097065.
- ↑ "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. November 2008. doi:10.2174/157489008786263970. PMID 18991792.
- ↑ "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 & Research 62 (11): 1588–1593. November 2010. doi:10.1002/acr.20275. PMID 20556817.
 |  |
