Formulation: A solid
Formal Name: N1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-amino-4-piperidinecarboxylic acid, trifluoroacetate salt
Purity: ≥98%
Formula Markup: C36H53N7O6 • XCF3COOH
Formula Weight: 679,9
Shelf life (days): 1460
CAS Number: 2767426-81-1
Notes: Difelikefalin is a κ-opioid receptor (KOR) agonist.{62330} It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively).