产品
编 号：F020577
分子式：C49H28F2N6Na6O23S6
分子量：1437.1
分子式：C49H28F2N6Na6O23S6
分子量：1437.1
产品类型
规格
价格
是否有货
1mg
询价
询价
结构图
CAS No: 104869-26-3
产品详情
生物活性：
NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 μM, 170 μM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 μM), P2Y2 (Ki=28.9 μM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).
体外研究：
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. 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).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.
NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 μM, 170 μM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 μM), P2Y2 (Ki=28.9 μM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).
体外研究：
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. 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).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.
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