Home Neuronal Signaling P2 Receptor antagonist Gefapixant For research use only.

Gefapixant

Synonyms: AF-219, MK-7264, R1646,RG-1646,RO 4926219

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

Gefapixant Chemical Structure

CAS No. 1015787-98-0

Purity & Quality Control

Batch: S666401 DMSO]71 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.88%
99.88

Gefapixant Related Products

Signaling Pathway

P2 Receptor Signaling Pathways

P2 Receptor Signaling Pathway

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
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05813223 Recruiting
Chronic Cough
Stuart Mazzone|Merck Sharp & Dohme LLC|Melbourne Health|Monash University|University of Melbourne
 January 1 2024 Early Phase 1
NCT03108924 Completed
Renal Insufficiency
Merck Sharp & Dohme LLC
 April 14 2017 Phase 1
NCT02790840 Completed
Healthy
Afferent Pharmaceuticals Inc. a subsidiary of Merck & Co. Inc. (Rahway New Jersey USA)
 May 16 2016 Phase 1
NCT02476890 Completed
Refractory Chronic Cough
Afferent Pharmaceuticals Inc. a subsidiary of Merck & Co. Inc. (Rahway New Jersey USA)
 October 28 2015 Phase 2
NCT02492776 Completed
Healthy
Afferent Pharmaceuticals Inc. a subsidiary of Merck & Co. Inc. (Rahway New Jersey USA)|Celerion
 July 7 2015 Phase 1
NCT02477709 Completed
Idiopathic Pulmonary Fibrosis
Afferent Pharmaceuticals Inc. a subsidiary of Merck & Co. Inc. (Rahway New Jersey USA)
 July 20 2015 Phase 2

Chemical Information & Solubility

Molecular Weight 353.40 Formula

C14H19N5O4S

 
CAS No. 1015787-98-0 SDF --
Smiles CC(C)C1=CC(=C(C=C1OC2=CN=C(N=C2N)N)S(=O)(=O)N)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 71 mg/mL ( (200.9 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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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.

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