Gefapixant

For research use only.

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

Gefapixant Chemical Structure

CAS No. 1015787-98-0

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.

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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

Solubility (25°C)

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

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 353.40
Formula

C14H19N5O4S

 

CAS No. 1015787-98-0
Storage powder
in solvent
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

In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

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Molecular Weight Calculator

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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

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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P2 Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID