Difelikefalin HCl

• Target :

  Others

• Related Pathways :

  Others

• Bioactivity :

  Difelikefalin HCl is a ?-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 HCl is selective for KOR over the ?-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) .

• Smiles :

  C([C@H](NC([C@H](NC([C@@H](CC1=CC=CC=C1)NC([C@@H](CC2=CC=CC=C2)N)=O)=O)CC(C)C)=O)CCCCN)(=O)N3CCC(C(O)=O)(N)CC3.Cl

• Molecular Formula :

  C36H53N7O6.xHCl

• Molecular Weight :

  789.237

• Shipping Conditions :

  Cool pack

• Storage Temperature :

  -20°C

• CAS Number :

  2711717-77-8