Difelikefalin TFA

CAT: 0931-T69530-01Size: 25 mgDry Ice: NoHazardous: No
CAT#:0931-T69530-01Size:25 mg
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CAS Number
2742623-88-5
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

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