产品
编 号:F741243
分子式:C23H24F2N4O4
分子量:458.46
产品类型
结构图
CAS No: 1621164-74-6
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产品详情
生物活性:
Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough.
体内研究:
Camlipixant (BLU-5937; 3-30 mg/kg; oral) 减少组胺和 ATP 诱导的豚鼠咳嗽过敏。Camlipixant (BLU-5937; 10-20 mg/kg; i.p.) 与对照动物相比,不会改变味觉知觉。Camlipixant (BLU-5937) 表现出优异的类药物特性,包括良好的口服生物利用度,在人体内预测清除率低,无血脑屏障渗透性,安全性高。Animal Model:Male Dunkin Hartley guinea pigs
Dosage:0.3, 3, 30 mg/kg
Administration:PO, approximately 2 h prior to tussive agent exposure
Result:Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs. Reduced significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs.
体外研究:
Camlipixant (BLU-5937; 500 nM) 阻断 ATP 介导的背根神经节 (DRG) 神经元敏化。