2417288-67-4

Name	1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)-
CAS	2417288-67-4
Molecular Formula	C24H26F2N4O3
MDL Number	MFCD32857164
Molecular Weight	456.48
MOL File	2417288-67-4.mol

Synonyms

1-Piperidinecarboxylic acid, 3-[[2-[2,6-difluoro-4-[(methylamino)carbonyl]phenyl]-7-methylimidazo[1,2-a]pyridin-3-yl]methyl]-, methyl ester, (3S)-

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Chemical Properties

density	1.34±0.1 g/cm3(Predicted)
form	Solid
pka	13.53±0.46(Predicted)
color	Off-white to light yellow

Hazard Information

Biological Activity

P2X3 antagonist 34 is a potent, selective, orally active P2X3 homotrimeric receptor antagonist with IC50 of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively . It is less active at human, rat and guinea pig P2X2/3 heterotrimeric receptors and has a strong antitussive effect.

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.

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.
It (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.

< table class="zh_use_1"> Animal Model: Male Dunkin Hartley guinea pigs Dosage: 0.3 mg/kg, 3 mg/kg, 30 mg/kg Administration: Oral administration Result: < td class="col2"> Significantly reduced the histamine-induced enhancement in the n umber of citric acid-induced coughs in a dose-dependent fashion.

target

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)

Supplier

ShangHai Caerulum Pharma Discovery Co., Ltd.

Telephone18149758185 18149758185

Websitehttp://www.caerulumpharma.com

ChemeGen(Shanghai) Biotechnology Co.,Ltd.

Telephone 18818260767

Websitehttp://www.chemegen.com

Beijing Jin Ming Biotechnology Co., Ltd.

Telephone010-60605840 15801484223;

Websitehttp://www.jm-bio.com/

TargetMol Chemicals Inc.

Telephone 4008200310

Websitehttps://www.targetmol.cn/

RD International Technology Co., Limited

Telephone 18024082417

Websitehttps://www.ruidiresearch.com

Wuhan Topule Biopharmaceutical Co., Ltd

Telephone +8618327326525

Websitehttp://topule.com/

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