KSC-12-192

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

Clinical data
Other names	"probe 1.1"
ATC code	None
Identifiers
IUPAC name 2-[4-(furan-2-ylmethyl)-5-[[4-methyl-3-(trifluoromethyl)phenyl]methylsulfanyl]-1,2,4-triazol-3-yl]pyridine
CAS Number	1526944-32-0 Y
PubChem CID	46245518
IUPHAR/BPS	9191
ChemSpider	58145205
ChEMBL	ChEMBL4458783
Chemical and physical data
Formula	C21H17F3N4OS
Molar mass	430.45 g·mol−1
3D model (JSmol)	Interactive image
SMILES CC1=C(C=C(C=C1)CSC2=NN=C(N2CC3=CC=CO3)C4=CC=CC=N4)C(F)(F)F
InChI InChI=1S/C21H17F3N4OS/c1-14-7-8-15(11-17(14)21(22,23)24)13-30-20-27-26-19(18-6-2-3-9-25-18)28(20)12-16-5-4-10-29-16/h2-11H,12-13H2,1H3 Key:OQJGZGAYSCWFCK-UHFFFAOYSA-N

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
		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

• Ketazocine
• RB-64
• ICI-199,441
• Spiradoline