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Gefapixant

Name: Gefapixant
Brand: TargetMol
SKU: T5099
Price: 32 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5099Cas No. 1015787-98-0

Alias RO 4926219, MK-7264, AF219

Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.

Gefapixant

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Purity: 99.50%

Catalog No. T5099Alias RO 4926219, MK-7264, AF219Cas No. 1015787-98-0

Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$32	In Stock	In Stock
5 mg	$53	In Stock	In Stock
10 mg	$77	In Stock	In Stock
25 mg	$158	In Stock	In Stock
50 mg	$255	In Stock	In Stock
100 mg	$377	In Stock	In Stock
200 mg	$536	-	In Stock

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

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:99.50%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
Targets&IC50	P2X2/3 heterotrimeric receptors (human):100-250 nM, Recombinant hP2X3 homotrimers:~30 nM
In vitro	The IC50 of Gefapixant has been reported as ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors, potencies very similar to those reported for recombinant rat receptors, and it displays no inhibitory impact on any non-P2X3 subunit-containing receptors (IC50 values>>10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5, and hP2X7 channels).
In vivo	In a rat model for knee osteoarthritis (developed 14 days after the intra-articular injection of monoiodoacetate), oral administration of Gefapixant twice daily for seven days resulted in a significant attenuation of weight bearing asymmetry, with a full reversal of observable hyperalgesia at the two higher doses [2].
Animal Research	A rodent model often employs for assessing the potential for drug effect in osteoarthritis (OA) pain is based on the intraarticular injection of monoiodoacetate (mIOA) into one knee joint of the rat. To measure the effect of Gefapixant on the weight bearing laterality and apparent hyperalgesia, Gefapixant is given by intraplantar or oral administration to the rats, with different concentrations (6, 20, and 60 mg/kg) two times a day and continues up to a week[2].
Synonyms	RO 4926219, MK-7264, AF219

Chemical Properties

Molecular Weight	353.4
Formula	C₁₄H₁₉N₅O₄S
Cas No.	1015787-98-0
Smiles	COc1cc(C(C)C)c(Oc2cnc(N)nc2N)cc1S(N)(=O)=O
Relative Density.	1.391 g/cm3 (Predicted)

Storage & Solubility Information

Storage

store at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 10 mg/mL (28.3 mM), pH is adjusted to 3 with HCl.

H2O: Insoluble

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.8297 mL	14.1483 mL	28.2965 mL	141.4827 mL
5 mM	0.5659 mL	2.8297 mL	5.6593 mL	28.2965 mL
10 mM	0.2830 mL	1.4148 mL	2.8297 mL	14.1483 mL
20 mM	0.1415 mL	0.7074 mL	1.4148 mL	7.0741 mL

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc