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CAS No. | 2742623-88-5 | Cat. No. | BCP44865 |
Name | Difelikefalin TFA | ||
Synonyms | CR845; CR 845; CR-845; FE 202845; FE202845; FE-202845; | ||
SMILES | N[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@@H](C(N1CCC(CC1)(C(O)=O)N)=O)CCCCN)=O)CC(C)C)=O)CC2=CC=CC=C2)=O)CC3=CC=CC=C3.OC(C(F)(F)F)=O | ||
Chemical Name | |||
Formula | C38H54F3N7O8 | M. Wt | 793.89 |
Purity | 98% | Storage | Store at 4-8°C |
Description | Difelikefalin 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 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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