Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NF157 significantly decreases the expression of metalloproteinase (MMP)-3, MMP-13, which can be used in the treatment of osteoarthritis (OA). NF157 is a highly selective nanomolar P2Y11 antagonist (pKi: 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.
产品描述 | NF157 significantly decreases the expression of metalloproteinase (MMP)-3, MMP-13, which can be used in the treatment of osteoarthritis (OA). NF157 is a highly selective nanomolar P2Y11 antagonist (pKi: 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. |
靶点活性 | P2Y1:1811 μM, P2Y1:187 μM(ki), P2Y2:170 μM, P2Y2:28.9 μM(ki), P2Y11:(ki)44.3 nM, P2Y11:(pki)7.35 , P2Y11:463 nM |
体外活性 | NF157 (30 and 60 μM; 24 hours) induces a significant reduction in the degradation of type II collagen in a dose-dependent manner. 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 (60 μM) nearly fully rescues type II collagen from degradation induced by TNF-α (10 ng/mL). NF157 shows 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][2]. |
分子量 | 1443.13 |
分子式 | C49H34F2N6Na6O23S6 |
CAS No. | 104869-26-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
NF157 104869-26-3 Immunology/Inflammation Neuroscience COX NF-157 NF 157 Inhibitor inhibitor inhibit