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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-P2X Receptor-BLU-5937
BLU-5937

Chemical Structure : BLU-5937

CAS No.: 1621164-74-6

BLU-5937 (Camlipixant, BLU5937)

货号: PC-20741Not For Human Use, Lab Use Only.

BLU-5937 (Camlipixant, BLU5937) is a potent, selective and non-competitive P2X3 homotrimeric receptor antagonist with IC50 of 25 and 92 nM for human and rat P2X3 receptors, repsectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

BLU-5937 (Camlipixant, BLU5937) is a potent, selective and non-competitive P2X3 homotrimeric receptor antagonist with IC50 of 25 and 92 nM for human and rat P2X3 receptors, repsectively.
BLU-5937 displays 1500-fold selectivity for human P2X3 over human P2X2/3.
BLU-5937 (500 nM) effectively inhibits P2X3-mediated sensitization of rat DRG neurons, blocks ATP-mediated neuron sensitization by inhibiting P2X3 homotrimeric receptors.
BLU-5937 (0.3-30 mg/kg, orally) reduces histamine- and ATP- induced cough hypersensitivity in guinea pigs.
BLU-5937 significantly reduced ATP- and histamineinduced enhancement in number of citric acid-induced coughs in the guinea pig.

物理化学性质&存储条件

分子量 458.47
分子式 C23H24F2N4O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

methyl (S)-2-((2-(2,6-difluoro-4-(methylcarbamoyl)phenyl)-7-methylimidazo[1,2-a]pyridin-3-yl)methyl)morpholine-4-carboxylate

参考文献

1. Garceau D, et al. Pulm Pharmacol Ther. 2019 Jun;56:56-62.

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