NF 157|104869-26-3|-陌孚医药/Medlife

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NF 157

目录号: PC12274 纯度: ≥98%

CAS No. :104869-26-3

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中文名称	NF 157
英文名称	NF 157
英文别名	1,3,5-Naphthalenetrisulfonicacid,8,8'-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-fluoro-3,1-phenylene)carbonylimino]]bis-,sodium salt (1:6);1,3,5-Naphthalenetrisulfonicacid,8,8'-[carbonylbis[imino-3,1-phenylenecarbonylimino(4-fluoro-3,1-phenylene)carbonylimino]]bis;CTK8E6694;NF 157;8,8'-[Carbonylbis[iMino-3,1-phenylenecarbonyliMino(4-fluoro-3,1-phenylene)carbonyliMino]]bis-1,3,5-naphthalenetrisulfonicacidhexasodiuMsalt
Cas No.	104869-26-3
分子式	C₄₉H₂₈N₆O₂₃F₂S₆-₆^.₆[Na+]
分子量	1437.10
包装储存	Please store the product under the recommended conditions in the Certificate of Analysis.

生物活性

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. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).

IC50 & Target[1][2]

pKi: 7.35 (P2Y11)
IC50: 463 nM (P2Y11), 1811 μM (P2Y1), 170 μM (P2Y2)
Ki: 44.3 nM (P2Y11), 187 μM (P2Y1), 28.9 μM (P2Y2)

体外研究(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.
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.

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

Western Blot Analysis

Cell Line:	SW1353 cells
Concentration:	30 and 60 μM
Incubation Time:	24 hours
Result:	Ameliorated TNF-α-induced degradation of type II collagen.

Western Blot Analysis

Cell Line:	SW1353 cells
Concentration:	30 and 60 μM
Incubation Time:	24 hours
Result:	Reduced TNF-α-induced activation of NF-κB.

运输条件

Room temperature or refrigerated transportation.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献

[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. [Information]

[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. [Information]

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