An acetamidophenylbutanoate derivative with inverse agonist and antagonist activity against human, but not mouse or rat, FFA2 (GPR43)
CATPB is an acetamidophenylbutanoate derivative with inverse agonist and antagonist activity against human, but not mouse or rat, FFA2 (GPR43). CATPB inhibits both constitutive and propionate (C3) -stimulated hFFA2 GTPγS incorporation (IC50 ~35 and 320 nM, respectively; [C3] = EC80, ~125 nM), as well as C3-induced hFFA2 G159E activity (IC50 ~400 nM). CATPB is shown to inhibit C3-induced intracellular ERK phosphorylation in hFFA2-expressing cells (IC50 ~3 μM against 10 mM C3).
International journal of immunopathology and pharmacology, 34, 2058738420958949-2058738420958949 (2020-12-30)
Neutrophils represent the first line of host cellular defense against various pathogens. The most recently described microbicidal mechanism of these cells is the release of neutrophil extracellular traps (NET). Currently, a wide range of chemical and biological stimuli are known
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