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P2X3 antagonist 34
Catalog No. T10560Cas No. 2417288-67-4
Alias 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].
P2X3 antagonist 34
Catalog No. T10560Alias BLU-5937Cas 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].
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 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
Chemical Properties
| 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 | P2X3 receptor (rat):92 nM , P2X2/3 heterotrimeric receptor (guinea pig):3450 nM , P2X2/3 heterotrimeric receptor (rat):1820 nM , P2X3 receptor (human):25 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 |
| Molecular Weight | 456.48 |
| Formula | C24H26F2N4O3 |
| Cas No. | 2417288-67-4 |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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