Difelikefalin TFA

  • Chemical Properties
CAS No. 2742623-88-5 Cat. No. BCP44865
Name Difelikefalin TFA
Synonyms CR845; CR 845; CR-845; FE 202845; FE202845; FE-202845;
Formula C38H54F3N7O8 M. Wt 793.89
  • Biological Activity
Description Difelikefalin is a κ-opioid receptor (KOR) agonist. 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).
Pathways Neuro Signaling Pathway Hormone Pathay GPCR/G Protein 
Targets Opioid Receptor 

Structure

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