Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Gefapixant (AF219) 是一个 P2X3 受体拮抗剂,其对人同源重组 hP2X3 和 hP2X2/3 的 IC50值分别是约 30 和 100-250 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 397 | 现货 | ||
2 mg | ¥ 571 | 现货 | ||
5 mg | ¥ 888 | 现货 | ||
10 mg | ¥ 1,310 | 现货 | ||
25 mg | ¥ 2,630 | 现货 | ||
50 mg | ¥ 3,930 | 现货 | ||
100 mg | ¥ 5,630 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 973 | 现货 |
产品描述 | Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors. |
靶点活性 | hP2X2/3 heterotrimeric receptors:100-250 nM, recombinant hP2X3 homotrimers:~30 nM |
体外活性 | The IC50 of Gefapixant has been reported as ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors, potencies very similar to those reported for recombinant rat receptors, and it displays no inhibitory impact on any non-P2X3 subunit-containing receptors (IC50 values>>10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5, and hP2X7 channels). |
体内活性 | In a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate), Gefapixant (7d bid, orally) attenuates the weight bearing laterality with a complete reversal of apparent hyperalgesia at the two higher doses [2]. |
动物实验 | A rodent model often employs for assessing the potential for drug effect in osteoarthritis (OA) pain is based on the intraarticular injection of monoiodoacetate (mIOA) into one knee joint of the rat. To measure the effect of Gefapixant on the weight bearing laterality and apparent hyperalgesia, Gefapixant is given by intraplantar or oral administration to the rats, with different concentrations (6, 20, and 60 mg/kg) two times a day and continues up to a week[2]. |
别名 | RO 4926219, AF219, MK-7264 |
分子量 | 353.4 |
分子式 | C14H19N5O4S |
CAS No. | 1015787-98-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: < 10 mM(< means unknown)
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.8297 mL | 14.1483 mL | 28.2965 mL | 70.7414 mL |
5 mM | 0.5659 mL | 2.8297 mL | 5.6593 mL | 14.1483 mL | |
10 mM | 0.283 mL | 1.4148 mL | 2.8297 mL | 7.0741 mL |
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。
Gefapixant 1015787-98-0 Membrane transporter/Ion channel Neuroscience P2X Receptor RO4926219 AF-219 RO 4926219 AF219 inhibit chronic cough MK 7264 AF 219 MK-7264 P2X3 knee osteoarthritis Inhibitor RO-4926219 MK7264 P2XRs inhibitor