NF546 is a selective agonist of non-nucleotide P2Y11(pEC50 of 6.27).

The selective non-nucleotide P2Y(11) agonist NF546 was identified.?NF546 had a pEC(50) of 6.27 and is relatively selective for P2Y(11) over P2Y(1), P2Y(2), P2Y(4), P2Y(6), P2Y(12), P2X(1), P2X(2), and P2X(2)-X(3).?The pA(2) of NF340 was 8.02 against ATPgammaS and 8.04 against NF546 (calcium assays).?NF546 was further tested for P2Y(11)-mediated effects in monocyte-derived dendritic cells.?Similarly to ATPgammaS, NF546 led to thrombospondin-1 secretion and inhibition of lipopolysaccharide-stimulated interleukin-12 release, whereas NF340 inhibited these effects.?Further, for the first time, it was shown that ATPgammaS or NF546 stimulation promotes interleukin 8 (IL-8) release from dendritic cells, which could be inhibited by NF340.