ChemicalBook CAS DataBase List 2417288-67-4

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

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

Uses

P2X3 antagonist 34 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. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect[1].

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)

IC 50

P2X3 Receptor

References

[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. DOI:10.1016/j.pupt.2019.03.007

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