Chemistry:3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol
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Short description: Chemical compound
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| Other names | 3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol |
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| Formula | C21H30O |
| Molar mass | 298.470 g·mol−1 |
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3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol is a synthetic, steroidal estrogen and a selective agonist of the ERβ.[1] It was discovered serendipitously and was the lead compound among a series of androsta-3,5-dienes as ERβ ligands.[1][2] Its affinity (IC50) for the ERβ was found to be 9 nM and it showed 62- and 160-fold binding selectivity for this receptor over the AR and the ERα, respectively.[1] The EC50 of the compound for the ERβ was found to be 69 nM and its intrinsic activity was 92% (relative to that of estradiol).[1] As such, it is a potent ERβ agonist with high affinity and selectivity.[1]
References
- ↑ 1.0 1.1 1.2 1.3 1.4 "Androstene-3,5-dienes as ER-beta selective SERMs". Bioorg. Med. Chem. Lett. 17 (22): 6295–8. 2007. doi:10.1016/j.bmcl.2007.09.001. PMID 17890084.
- ↑ "Estrogen, vascular estrogen receptor and hormone therapy in postmenopausal vascular disease". Biochem. Pharmacol. 86 (12): 1627–42. 2013. doi:10.1016/j.bcp.2013.09.024. PMID 24099797.
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