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].

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]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

1437.10

C₄₉H₂₈F₂N₆Na₆O₂₃S₆

104869-26-3

固体

Off-white to pink

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Ullmann H, et al. Synthesis and structure-activity relationships of suramin-derived P2Y11 receptor antagonists with nanomolar potency. J Med Chem. 2005 Nov 3;48(22):7040-8.  [Content Brief]

  [2]. Wang D, et al. Inhibition of P2Y11R ameliorated TNF-α-induced degradation of extracellular matrix in human chondrocytic SW1353 cells. Am J Transl Res. 2019 Apr 15;11(4):2108-2116.  [Content Brief]