BLU-5937
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- CAS号:
- 2417288-67-4
- 英文名:
- 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)-
- 英文别名:
- 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)-
- 中文名:
- BLU-5937
- 中文别名:
- 化合物 T10560;化合物 P2X3 ANTAGONIST 34
- CBNumber:
- CB58186525
- 分子式:
- C24H26F2N4O3
- 分子量:
- 456.48
- MOL File:
- 2417288-67-4.mol
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BLU-5937化学性质
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密度:
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1.34±0.1 g/cm3(Predicted)
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酸度系数(pKa):
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13.53±0.46(Predicted)
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形态:
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Solid
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颜色:
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Off-white to light yellow
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BLU-5937性质、用途与生产工艺
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。
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)
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.
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.
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Animal Model:
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Male Dunkin Hartley guinea pigs
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Dosage:
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0.3 mg/kg, 3 mg/kg, 30 mg/kg
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Administration:
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Oral administration
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Result:
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Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs in a dose-dependent fashion.
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BLU-5937
上下游产品信息
上游原料
下游产品
2417288-67-4, BLU-5937 相关搜索:
- 抑制剂
- 医药原料
- 化合物 P2X3 ANTAGONIST 34
- 化合物 T10560
- 2417288-67-4
- 1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)-