NF157

NF157 is a highly selective nanomolar P2Y11 antagonist with a pK_i of 7.35. The IC₅₀s are 463 nM, 1811 µM, 170 µM for P2Y11 (K_i=44.3 nM), P2Y1 (K_i=187 µM), P2Y2 (K_i=28.9 µM), respectively^[1]. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA)^[2]. IC50 & Target: pKi: 7.35 (P2Y11)^[1]
IC50: 463 nM (P2Y11), 1811 µM (P2Y1), 170 µM (P2Y2)^[1]
Ki: 44.3 nM (P2Y11), 187 µM (P2Y1), 28.9 µM (P2Y2)^[1] In Vitro: NF157 displays selectivity for P2Y11 over P2Y1 (>650-fold), P2Y2 (>650-fold), P2X2 (3-fold), P2X3 (8-fold), P2X4 (>22-fold), and P2X7 (>67-fold) but no selectivity over P2X1^[1].
NF157 (30 and 60 µM; 24 hours) causes a significant reduction in degradation of type II collagen in a dose-dependent manner. 60 µM NF157 nearly completely rescues type II collagen from degradation induced by TNF-α (10 ng/mL)^[2].
NF157 (30 and 60 µM; 24 hours) almost fully restores nuclear translocation of p65 triggered by TNF-α (10 ng/mL) and significantly reduces the luciferase activity of NF-κB^[2].