KOR agonist 6

KOR agonist 6 (Compound 5i) exhibits ultra-high binding affinity to κ-opioid receptor (KOR (K_i = 0.00025 nM)) and exceptional subtype selectivity over μ-opioid receptor (MOR (K_i = 14.1 nM)) and δ-opioid receptor (DOR (K_i = 120.7nM))^[1].
KOR agonist 6 shows agonistic activity at MOR (EC₅₀ = 44.78 nM, E_max = 88.71%) and DOR (EC₅₀ = 15.26 nM, E_max = 85.16%) in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation (EC₅₀ = 200.3 nM, E_max = 99.51%)^[1].
KOR agonist 6 stimulates KOR-mediated [³⁵S]GTPγS binding with potent activity (EC₅₀ = 0.024 nM, E_max = 106.9%) in KOR-expressing cell membranes, inhibits cAMP accumulation in KOR-expressing HEK293 cells with ultra-potent agonistic activity (EC₅₀ = 0.43 pM, E_max = 63.63%) and induces β-arrestin recruitment in KOR-Tango plasmid-transfected HTLA cells with lower potency (EC₅₀ = 0.143 nM, E_max = 42.89%)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .