Difelikefalin HCl
Product Specifications
CAS Number
2711717-77-8
Target
Others
Related Pathways
Others
Bioactivity
Difelikefalin HCl 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 HCl 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) .
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
Ice Packs
Storage Temperature
-20°C
Available Sizes
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