NF157

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NF157

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

104869-26-3

NF157 是一种高度选择性的P2Y11拮抗剂，pK_i为 7.35。对 P2Y11 (K_i=44.3 nM)，P2Y1 (K_i=187 μM)，P2Y2 (K_i=28.9 μM) 的IC₅₀分别为 463 nM，1811 μM， 170 μM。NF157 能显着降低金属蛋白酶 (MMP)-3，MMP-13 的表达，可用于骨关节炎的研究。

生物活性

NF157 is a highly selective nanomolarP2Y11antagonist with apK_iof 7.35. TheIC₅₀s 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]

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^[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].

Western Blot Analysis^[2]

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^[2]

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

分子量

1437.10

Formula

C₄₉H₂₈F₂N₆Na₆O₂₃S₆

CAS 号

104869-26-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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