Home Neuronal Signaling P2 Receptor antagonist Gefapixant

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Gefapixant P2 Receptor antagonist

Cat.No.S6664

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. This compound has shown promise for the treatment of refractory and unexplained chronic cough.
Gefapixant P2 Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 353.40

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 71 mg/mL (200.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous 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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Chemical Information, Storage & Stability

Molecular Weight 353.40 Formula

C14H19N5O4S

 

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1015787-98-0 -- Storage of Stock Solutions

Synonyms AF-219, MK-7264, R1646,RG-1646,RO 4926219 Smiles CC(C)C1=CC(=C(C=C1OC2=CN=C(N=C2N)N)S(=O)(=O)N)OC

Mechanism of Action

Targets/IC50/Ki
hP2X3
(Cell-free assay)
30 nM
hP2X2/3
(Cell-free assay)
100-250 nM
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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