Chemistry:Β-LGND2
From HandWiki
Short description: Chemical compound
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| Other names | β-LGND2; ER-β-selective ligand 2 |
| Drug class | Nonsteroidal estrogen; Selective ERβ agonist |
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| Formula | C15H10BrNO4 |
| Molar mass | 348.152 g·mol−1 |
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β-LGND2, also known as ERβ-selective ligand 2 or as GTx-878, is a synthetic nonsteroidal estrogen and selective ERβ agonist which was under development by GTx for the treatment of benign prostatic hyperplasia, prostatitis, and rheumatoid arthritis but was never marketed.[1][2][3][4][5][6] It shows approximately 25-fold selectivity for activation of the ERβ over the ERα (EC50 = 2 nM and 52 nM, respectively).[3] β-LGND2 is an isoquinolinone derivative.[2][5]
References
- ↑ "Research programme: Estrogen receptor beta agonists - Oncternal Therapeutics - AdisInsight". https://adisinsight.springer.com/drugs/800027855.
- ↑ 2.0 2.1 "Estrogen receptor-{beta}-selective ligands alleviate high-fat diet- and ovariectomy-induced obesity in mice". J. Biol. Chem. 285 (41): 31292–303. October 2010. doi:10.1074/jbc.M110.147850. PMID 20657011.
- ↑ 3.0 3.1 "Pharmacologic activation of estrogen receptor β increases mitochondrial function, energy expenditure, and brown adipose tissue". FASEB J. 31 (1): 266–281. January 2017. doi:10.1096/fj.201600787RR. PMID 27733447. "We found that β-LGND2, also known as GTx-878 (GTx, Inc. (31)), reduces body weight and fat mass without altering feed consumption of high-fat diet (HFD)-fed WT, but not ER-βKO, mice.".
- ↑ "β-LGND2, an ERβ selective agonist, inhibits pathologic retinal neovascularization". Invest. Ophthalmol. Vis. Sci. 53 (8): 5066–75. July 2012. doi:10.1167/iovs.12-9627. PMID 22714897.
- ↑ 5.0 5.1 "Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential". Steroids 90: 13–29. November 2014. doi:10.1016/j.steroids.2014.06.012. PMID 24971815.
- ↑ "Estrogen receptor beta selective nonsteroidal estrogens: seeking clinical indications". Expert Opin Ther Pat 20 (4): 507–34. April 2010. doi:10.1517/13543771003657164. PMID 20302450.
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