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).
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).
Ferritin is a protein of 450 kDa consisting of 24 subunits that is present in every cell type. Invertebrates, these subunits are both the light (L) and the heavy (H) type with an apparent molecular weight of 19 kDA or 21 kDA respectively. The ferritin fou
Petunidin-3-O-glucoside chloride has significantly higher antioxidant activity than the Fe2+ control. Petunidin-3-O-glucoside causes problems in digestibility, may be important dietary supplements with beneficial health effects.