A κ-opioid receptor agonist
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Difelikefalin (trifluoroacetate salt)

Item No. 34542

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1-(D-phenylalanyl-D-phenylalanyl-D-leucyl-D-lysyl)-4-amino-4-piperidinecarboxylic acid, trifluoroacetate salt
CAS Number
2767426-81-1
Synonyms
  • CR845
  • FE 202845
Molecular Formula
C36H53N7O6 • XCF3COOH
Formula Weight
679.9
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Ethanol: soluble
SMILES
N[C@H](CC1=CC=CC=C1)C(N[C@H](CC2=CC=CC=C2)C(N[C@H](CC(C)C)C(N[C@H](CCCCN)C(N3CCC(N)(CC3)C(O)=O)=O)=O)=O)=O.OC(C(F)(F)F)=O
InChi Code
InChI=1S/C36H53N7O6.C2HF3O2/c1-24(2)21-29(32(45)40-28(15-9-10-18-37)34(47)43-19-16-36(39,17-20-43)35(48)49)42-33(46)30(23-26-13-7-4-8-14-26)41-31(44)27(38)22-25-11-5-3-6-12-25;3-2(4,5)1(6)7/h3-8,11-14,24,27-30H,9-10,15-23,37-39H2,1-2H3,(H,40,45)(H,41,44)(H,42,46)(H,48,49);(H,6,7)/t27-,28-,29-,30-;/m1./s1
InChi Key
DNTIYNDNHLWSLZ-KGURMGBCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $121

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    5 mg

    $505

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    10 mg

    $894

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    Product Description

    Difelikefalin is a κ-opioid receptor (KOR) agonist.1 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).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Schteingart, C.D., Menzaghi, F., Jiang, G., et al. Synthetic peptide amides. (2008).