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