Chemistry:KSC-12-192
From HandWiki
Short description: KOR biased agonist.
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| Other names | "probe 1.1" |
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| Formula | C21H17F3N4OS |
| Molar mass | 430.45 g·mol−1 |
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KSC-12-192 is a drug that is used in scientific research to study the κ-opioid receptor, where it acts as a biased agonist.[1]
KSC-12-192 preferentially activates G-protein coupling over β-arrestin 2 recruitment in vitro, an intrinsic activity shared with many other KOR ligands developed to separate KOR-mediated analgesia from accompanying dysphoria.
Compared with most of the known KOR G-protein biased agonists, KSC-12-192 and its parent compound ML138 do not exhibit stereoisomerism.
Out of a range of tested compounds with the same substituted triazole scaffold (see table), KSC-12-192 had the highest reported in vitro potency as a human KOR agonist (EC50 = 31nM[2]).
| Scaffold | Identifiers | X | R1 | R2 | R3 | |
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KSC-12-192 | O | H | CH3 | CF3 | |
| ML138 | KSC-5-240 | O | H | Cl | Cl | |
| KSC-12-193 | S | H | CH3 | CF3 | ||
| KSC-5-247G | S | H | Cl | Cl | ||
| KSC-12-238-B5 | O | CH3 | CH3 | CF3 | ||
| KSC-12-238-B4 | O | CH3 | Cl | Cl | ||
See also
References
- ↑ "Development of functionally selective, small molecule agonists at kappa opioid receptors". The Journal of Biological Chemistry 288 (51): 36703–36716. December 2013. doi:10.1074/jbc.M113.504381. PMID 24187130.
- ↑ "Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential". Journal of Medicinal Chemistry 61 (22): 9841–9878. November 2018. doi:10.1021/acs.jmedchem.8b00435. PMID 29939744.
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