Gefapixant

Catalog No.S6664 Synonyms: AF-219, MK-7264, R1646,RG-1646,RO 4926219

For research use only.

Gefapixant (AF-219, MK-7264, R1646, RG-1646, RO 4926219) is an orally active small molecule antagonist of human P2X3 receptor with IC50 of about 30 nM, 100–250 nM for recombinant hP2X3 homotrimers and hP2X2/3 heterotrimeric receptors, respectively. Gefapixant has shown promise for the treatment of refractory and unexplained chronic cough.

Gefapixant Chemical Structure

CAS No. 1015787-98-0

Purity & Quality Control

Choose Selective P2 Receptor Inhibitors

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Biological Activity

Description Gefapixant (AF-219, MK-7264, R1646, RG-1646, RO 4926219) is an orally active small molecule antagonist of human P2X3 receptor with IC50 of about 30 nM, 100–250 nM for recombinant hP2X3 homotrimers and hP2X2/3 heterotrimeric receptors, respectively. Gefapixant has shown promise for the treatment of refractory and unexplained chronic cough.
Targets
hP2X3 [1]
(Cell-free assay)
hP2X2/3 [1]
(Cell-free assay)
30 nM 100-250 nM

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 71 mg/mL
(200.9 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 353.40
Formula

C14H19N5O4S

 

CAS No. 1015787-98-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)C1=CC(=C(C=C1OC2=CN=C(N=C2N)N)S(=O)(=O)N)OC

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03108924 Completed Drug: Gefapixant Renal Insufficiency Merck Sharp & Dohme Corp. April 14 2017 Phase 1
NCT02790840 Completed Drug: Omeprazole|Drug: Gefapixant Healthy Afferent Pharmaceuticals Inc. May 16 2016 Phase 1
NCT02476890 Completed Drug: Gefapixant 100 mg|Drug: Placebo Refractory Chronic Cough Afferent Pharmaceuticals Inc. October 28 2015 Phase 2
NCT02492776 Completed Drug: Omeprazole|Drug: Gefapixant Healthy Afferent Pharmaceuticals Inc.|Celerion July 7 2015 Phase 1
NCT02477709 Completed Drug: Gefapixant Idiopathic Pulmonary Fibrosis Afferent Pharmaceuticals Inc. July 20 2015 Phase 2
NCT02229877 Completed Drug: Omeprazole|Drug: Gefapixant Healthy Volunteers Afferent Pharmaceuticals Inc.|Celerion October 6 2014 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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