P2X3 antagonist 34

Name: P2X3 antagonist 34
Brand: TargetMol
SKU: T10560
Rating: 4.5 (1 reviews)

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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

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Catalog No. T10560Alias BLU-5937Cas No. 2417288-67-4

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

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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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	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.
Synonyms	BLU-5937

Chemical Properties

Molecular Weight	456.48
Formula	C₂₄H₂₆F₂N₄O₃
Cas No.	2417288-67-4
Smiles	CNC(=O)c1cc(F)c(-c2nc3cc(C)ccn3c2C[C@@H]2CCCN(C2)C(=O)OC)c(F)c1
Relative Density.	1.34 g/cm3 (Predicted)

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Storage

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

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

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