P2X3 antagonist 34|2417288-67-4|-陌孚医药/Medlife

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P2X3 antagonist 34

目录号: PL08677 纯度: ≥99%

CAS No. :2417288-67-4

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中文名称	P2X3 antagonist 34
英文名称	P2X3 antagonist 34
英文别名	P2X3 antagonist 34;GTPL11232;BLU5937;NEO5937;methyl (3S)-3-[[2-[2,6-difluoro-4-(methylcarbamoyl)phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]piperidine-1-carboxylate
Cas No.	2417288-67-4
分子式	C₂₄H₂₆F₂N₄O₃
分子量	456.49
包装储存	-20°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

产品详情	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。
生物活性	P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC 50 s 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.
性状	Solid
IC50 & Target[1][2]	IC50: 25?nM (Human P2X3 receptor), 92?nM (Rat P2X3 receptor)and 126?nM (Guinea pig P2X3 receptor), 1820 nM (Rat P2X2/3 heterotrimeric receptor) and 3450 nM (Guinea pig P2X2/3 heterotrimeric receptor)
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	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 fashion in a guinea pig cough model. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献	[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.

溶解度数据	In Vitro: DMSO : 100 mg/mL (219.06 mM; Need ultrasonic)配制储备液

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