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P2X3 antagonist 34

Catalog No. T10560 CAS 2417288-67-4

Synonyms: BLU-5937

P2X3 antagonist 34, a potent, selective, and orally active antagonist, targets the P2X3 homotrimeric receptor, exhibiting IC50s of 25 nM, 92 nM, and 126 nM for human, rat, and guinea pig P2X3 receptors respectively. It shows reduced activity against P2X2/3 heterotrimeric receptors across human, rat, and guinea pig models. Notably, this compound demonstrates a significant anti-tussive effect without altering taste[1].

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P2X3 antagonist 34, CAS 2417288-67-4

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 1,080.00
50 mg	8-10 weeks	$ 1,410.00
100 mg	8-10 weeks	$ 2,150.00

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Description	P2X3 antagonist 34, a potent, selective, and orally active antagonist, targets the P2X3 homotrimeric receptor, exhibiting IC50s of 25 nM, 92 nM, and 126 nM for human, rat, and guinea pig P2X3 receptors respectively. It shows reduced activity against P2X2/3 heterotrimeric receptors across human, rat, and guinea pig models. Notably, this compound demonstrates a significant anti-tussive effect without altering taste[1].
Targets&IC50	P2X2/3 heterotrimeric receptor (rat):1820 nM , P2X3 receptor (human):25 nM , P2X2/3 heterotrimeric receptor (guinea pig):3450 nM , P2X3 receptor (rat):92 nM
In vitro	P2X3 antagonist 34 (BLU-5937; 500 nM) effectively inhibits αβ-meATP-induced sensitization and the resultant firing activity in isolated primary nociceptors within rat dorsal root ganglions (DRGs) by antagonizing P2X3 homotrimeric receptors. Both the sensitization caused by αβ-meATP and the inhibition by P2X3 antagonist 34 are reversible following washout [1].
In vivo	Treatment with the P2X3 antagonist 34 (BLU-5937; administered orally at doses ranging from 0.3 to 30 mg/kg in male Dunkin Hartley guinea pigs) significantly and dose-dependently diminished both histamine-induced and ATP-induced enhancements of citric acid-induced coughs in a guinea pig cough model. This outcome highlights the compound's efficacy in reducing cough reflex sensitivity through oral administration.

Synonyms	BLU-5937
Molecular Weight	456.48
Formula	C24H26F2N4O3
CAS No.	2417288-67-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Keywords

P2X3 antagonist 34 2417288-67-4 BLU 5937 BLU-5937 P-2X3 antagonist 34 BLU5937 inhibitor inhibit

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