Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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].
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
25 mg | 8-10 weeks | $ 1,080.00 | |
50 mg | 8-10 weeks | $ 1,410.00 | |
100 mg | 8-10 weeks | $ 2,150.00 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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P2X3 antagonist 34 2417288-67-4 BLU 5937 BLU-5937 P-2X3 antagonist 34 BLU5937 inhibitor inhibit