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104869-26-3 | NF157

NF157 NLT 98%

SKU : MC504099

CAS Number : 104869-26-3

Molecular Formula : C49H28F2N6Na6O23S6 | Molecular Weight : 1437.10

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Purity NLT 98%
Storage at 20ºC 2 years

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Chemical Name NF157
CAS Number 104869-26-3
MDL Number MFCD09971078
Molecular Formula C49H28F2N6Na6O23S6
Molecular Weight 1437.10
Introduction of 104869-26-3 :

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[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].

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