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P2X3 antagonist 34

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P2X3 antagonist 34

Catalog No. T10560Cas No. 2417288-67-4

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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Pack Size	Price	Availability
25 mg	$1,080	8-10 weeks
50 mg	$1,410	8-10 weeks
100 mg	$2,150	8-10 weeks

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Product Introduction

Bioactivity

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 (rat):92 nM , P2X3 receptor (human):25 nM , P2X2/3 heterotrimeric receptor (guinea pig):3450 nM
In vitro	P2X3 antagonist 34 (BLU-5937; 500 nM) effectively inhibits αβ-meATP-induced sensitization and the consequent 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.
Alias	BLU-5937

Chemical Properties

Molecular Weight	456.48
Formula	C24H26F2N4O3
Cas No.	2417288-67-4

Storage & Solubility Information

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

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Keywords

P2X3 antagonist 34BLU 5937P-2X3 antagonist 34BLU5937