OSU-ERβ-12
 Hydrogen atoms bonded to boron are omitted for clarity. | |
| Clinical data | |
|---|---|
| Other names | OSU-ERb-12; WT-IV-12[1] |
| Drug class | Selective ERβ agonist |
| Identifiers | |
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| CAS Number | |
| Chemical and physical data | |
| Formula | C15H30B10O2 |
| Molar mass | 350.50 g·mol−1 |
| 3D model (JSmol) | |
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OSU-ERβ-12 is a highly selective estrogen receptor beta (ERβ) full agonist which is under investigation for potential medical use, such as treatment of fibrosis.[2][3][4][1][unreliable source?]
Pharmacology
[edit]While OSU-ERβ-12 displays only a 3-fold binding selectivity for ERβ over the estrogen receptor alpha (ERα), it shows more than a 100-fold functional selectivity for ERβ over ERα, with EC50 values of 19–78 nM and 3,828–30,000 nM, respectively.[2][1][4] The drug shows good drug-like properties and had superior pharmacokinetic properties to those of the earlier ERβ agonist erteberel (LY-500307) in preclinical research.[2] It produces anti-fibrotic effects in rodents.[2][1]
Chemistry
[edit]The chemical synthesis of OSU-ERβ-12 has been described.[2][4] Various analogues of OSU-ERβ-12 have been described.[4] OSU-ERβ-12 has an unusual para-carborane chemical structure.[2][4][3]
History
[edit]It was first described in the scientific literature by 2020.[1][2] The drug was developed by W. Tjarks and colleagues at Ohio State University.[1][4]
See also
[edit]References
[edit]- 1 2 3 4 5 6 Klein A (December 2020). Novel Selective Estrogen Receptor Modulator (SERM) OSU-ERβ-12 Demonstrates Anti-fibrotic Efficacy (Honors Research Thesis thesis). The Ohio State University.
- 1 2 3 4 5 6 7 Young GM, Helms TH, Kulp SK, Adeluola AA, Radomska HS, Wilson TA, et al. (November 2025). "OSU-ERβ-12: a promising pre-clinical candidate selective estrogen receptor beta agonist". Scientific Reports. 15 (1) 38377. doi:10.1038/s41598-025-22258-x. PMC 12583746. PMID 41184385.
- 1 2 Adeluola AA, Radomska HS, Wilson TA, Kulp SK, Kabat A, Helms TH, et al. (January 2025). "The elucidation of species-specific receptor pharmacology: A case study using subtype-selective para- and meta-carborane estrogen receptor agonists". The Journal of Pharmacology and Experimental Therapeutics. 392 (1) 100001. doi:10.1124/jpet.123.001874. PMID 39892992.
- 1 2 3 4 5 6 Sedlák D, Wilson TA, Tjarks W, Radomska HS, Wang H, Kolla JN, et al. (July 2021). "Structure-Activity Relationship of para-Carborane Selective Estrogen Receptor β Agonists". Journal of Medicinal Chemistry. 64 (13): 9330–9353. doi:10.1021/acs.jmedchem.1c00555. PMID 34181409.
