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P2X3 antagonist 34

Catalog No. T10560   CAS 2417288-67-4
Synonyms: BLU-5937

P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC 50 s 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 and no taste alteration[1].

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P2X3 antagonist 34 Chemical Structure
P2X3 antagonist 34, CAS 2417288-67-4
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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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Biological Description
Chemical Properties
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Description P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC 50 s 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 and no taste alteration[1].
Targets&IC50 Rat P2X2/3 heterotrimeric receptor:1820 nM , Human P2X3 receptor:25 nM , Guinea pig P2X2/3 heterotrimeric receptor:3450 nM , P2X3 receptor (rat):92 nM
In vitro P2X3 antagonist 34 (BLU-5937; 500 nM) can 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 [1].
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 manner in a guinea pig cough model [1]. P2X3 antagonist 34 (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 [1]. Animal Model: Male Dunkin Hartley guinea pigs [1] Dosage: 0.3 mg/kg, 3 mg/kg, 30 mg/kg Administration: Oral administration Result: Significantly reduced the histamine-induced enhancement in the number of citric acid-induced coughs in a dose-dependent fashion.
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

TargetMolReferences 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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