| CAS NO: | 2417288-67-4 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
BLU-5937 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。BLU-5937 对人，大鼠和豚鼠 P2X2/3 异三聚体受体的活性较低。BLU-5937 具有很强的镇咳作用。
| Cas No. | 2417288-67-4 |
| 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 |
| 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 |
| 产品描述 | BLU-5937 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. BLU-5937 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. BLU-5937 has strong anti-tussive effect[1]. 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 BLU-5937 are reversible after washout[1]. 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].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. |
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