Difelikefalin (CR-845; FE-202845) is a peripherally restricted, selective agonist of the kappa opioid receptor (KOR). It exhibits anti-inflammatory properties and holds promise for modulating pruritus in conditions associated with chronic kidney disease.
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).
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).
RK-52 is a synthetic inhibitor of rhodesain, characterized by an impressive ksecond value (ksecond = 67000 × 103 M−1 min−1) and by a picomolar affinity toward the trypanosomal protease (Ki = 38 pM).
11(Z),14(Z),17(Z)-Eicosatrienoic acid methyl ester is the ester derivative of 11(Z),14(Z),17(Z)-eicosatrienoic acid, identified within lipid-producing microalgae Nannochloropsis, as well as in diesel-contaminated soils and residential wastewater.
All-cis-4,7,10,13,16-Docosapentaenoic acid ethyl ester (all-cis-4,7,10,13,16-DPA ethyl ester) is a derivative of docosapentaenoic acid (DPA), an omega-3 fatty acid prevalent in fish oils. This ethyl ester form is commonly included in dietary supplements formulations to enhance omega-3 fatty acid intake.