Difelikefalin TFA - CAS 2742623-88-5

Difelikefalin TFA 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 TFA 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) .

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Others

2742530

C42H56F9N7O12

1021.92

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

-20°C

Ice Packs

Small Compound