Powder: -20°C for 3 years | In solvent: -80°C for 1 year
P2X3 antagonist 34 是一种对P2X3同型三聚体受体具有高效性、选择性和口服活性的拮抗剂,其IC50值针对人类P2X3、大鼠P2X3及豚鼠P2X3分别为25 nM、92 nM和126 nM。相比之下,该化合物对人类、大鼠和豚鼠的P2X2/3异三聚体受体展现低活性。P2X3 antagonist 34 显著具有抗咳功效,同时不会影响味觉。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
25 mg | ¥ 10,800 | 8-10周 | ||
50 mg | ¥ 14,100 | 8-10周 | ||
100 mg | ¥ 21,600 | 8-10周 |
P2X3 antagonist 34 的其他形式现货产品:
产品描述 | P2X3 antagonist 34, a potent, selective, and orally active antagonist, targets the P2X3 homotrimeric receptor, exhibiting IC50s of 25 nM, 92 nM, and 126 nM for human, rat, and guinea pig P2X3 receptors respectively. It shows reduced activity against P2X2/3 heterotrimeric receptors across human, rat, and guinea pig models. Notably, this compound demonstrates a significant anti-tussive effect without altering taste[1]. |
靶点活性 | P2X2/3 heterotrimeric receptor (rat):1820 nM , P2X3 receptor (human):25 nM , P2X2/3 heterotrimeric receptor (guinea pig):3450 nM , P2X3 receptor (rat):92 nM |
体外活性 | P2X3 antagonist 34 (BLU-5937; 500 nM) can block αβ-meATP-induced sensitization and firing activity of isolated primary nociceptors in rat dorsal root ganglions (DRGs), through P2X3 homotrimeric receptor antagonism. The sensitizing effect of αβ-meATP and the inhibition of P2X3 antagonist 34 are reversible after washout [1]. |
体内活性 | P2X3 antagonist 34 (BLU-5937; 0.3-0 mg/kg, oral administration; male Dunkin Hartley guinea pigs) treatment significantly reduces the histamine-induced enhancement in the number of citric acid-induced coughs in a dose-dependent manner in a guinea pig cough model [1]. P2X3 antagonist 34 (BLU-5937; 3 and 30 mg/kg, oral) is also shown to reduce significantly and dose-dependently the ATP-induced enhancement of citric acid-induced coughs in the guinea pig [1]. Animal Model: Male Dunkin Hartley guinea pigs [1] Dosage: 0.3 mg/kg, 3 mg/kg, 30 mg/kg Administration: Oral administration Result: Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs in a dose-dependent fashion. |
别名 | BLU-5937 |
分子量 | 456.48 |
分子式 | C24H26F2N4O3 |
CAS No. | 2417288-67-4 |
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。
P2X3 antagonist 34 2417288-67-4 BLU 5937 BLU-5937 P-2X3 antagonist 34 BLU5937 Inhibitor inhibitor inhibit