Difelikefalin TFA

• Target:

  Others

• Related Pathways:

  Others

• Bioactivity:

  Difelikefalin TFA 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 TFA 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(O)=O)(F)(F)F.C(C(O)=O)(F)(F)F.C(C(O)=O)(F)(F)F.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

• Molecular Formula:

  C42H56F9N7O12

• Molecular Weight:

  1021.92

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2742623-88-5