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P2X3 antagonist 34

目录号 : GC60281

P2X3 antagonist 34 是一种有效的,选择性的,口服活性的 P2X3 同型三聚体受体拮抗剂,对人 P2X3,大鼠 P2X3 和豚鼠 P2X3 受体的 IC50 分别为 25 nM,92 nM 和 126 nM。P2X3 antagonist 34 对人,大鼠和豚鼠 P2X2/3 异三聚体受体的活性较低。P2X3 antagonist 34 具有很强的镇咳作用。

规格 价格 库存 购买数量
5mg
¥3,150.00
现货
10mg
¥5,400.00
现货
50mg
¥15,300.00
现货
100mg
¥23,400.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

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产品描述

P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25?nM, 92?nM and 126?nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect[1].

P2X3 antagonist 34 (BLU-5937; 500?nM) is able to 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].

P2X3 antagonist 34 (BLU-5937; 0.3-0mg/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 fashion in a guinea pig cough model[1].P2X3 antagonist 34 (BLU-5937; 3 and 30mg/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]

[1]. Garceau D, et al. BLU-5937: A selective P2X3 antagonist with potent anti-tussive effect and no taste alteration. Pulm Pharmacol Ther. 2019 Jun;56:56-62.

Chemical Properties

Cas No. N/A SDF
别名 N/A
化学名 N/A
Canonical SMILES O=C(OC)N1C[C@@H](CCC1)CC2=C(N=C3C=C(C=CN32)C)C4=C(C=C(C=C4F)C(NC)=O)F
分子式 C24H26F2N4O3 分子量 456.49
溶解度 N/A 储存条件 -20°C, protect from light
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

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