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Ligand-gated ion channels
P2X receptors
Gefapixant - 98%, high purity , CAS No.1015787-98-0, Antagonist of P2X3

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Gefapixant - 98%, high purity , CAS No.1015787-98-0, Antagonist of P2X3

Moligand™
≥98%

CAS#: 1015787-98-0
Formula: C₁₄H₁₉N₅O₄S
Molecular Weight: 353.4
EC Number: 823-334-6
PubChem CID: 24764487

Item Number

G413575

Grouped product items
SKU	Size	Availability	Price
G413575-5mg	5mg	In stock	$107.90
G413575-10mg	10mg	In stock	$157.90
G413575-25mg	25mg	In stock	$315.90
G413575-50mg	50mg	In stock	$513.90
G413575-100mg	100mg	In stock	$840.90

P2 Receptor Antagonists

View related series

P2X3 Antagonist

Basic Description

Synonyms	Gefapixant\|1015787-98-0\|AF-219\|Gefapixant [USAN]\|RO4926219\|Benzenesulfonamide, 5-[(2,4-diamino-5-pyrimidinyl)oxy]-2-methoxy-4-(1-methylethyl)-\|RG-1646\|Ro-4926219\|6K6L7E3F1L\|R-1646\|AF219\|Gefapixant(AF-219,MK-7264)\|RG1646\|5-[(2,4-diaminopyrimidin-5-yl)oxy]-
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	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. Gefapi
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ANTAGONIST
Mechanism of action	Antagonist of P2X3
Product Description	Information Gefapixant 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 (Cell-free assay); hP2X2/3 (Cell-free assay) 30 nM; 100-250 nM

Product Properties

ALogP	1.061
HBD Count	3
Rotatable Bond	5

Associated Targets

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

P2RX3 Tclin P2X purinoceptor 3 1 Activities

Discover Target: P2RX3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

P2RX2 Tchem P2X purinoceptor 2 0 Activities

Discover Target: P2RX2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	5-(2,4-diaminopyrimidin-5-yl)oxy-2-methoxy-4-propan-2-ylbenzenesulfonamide
INCHI	InChI=1S/C14H19N5O4S/c1-7(2)8-4-10(22-3)12(24(17,20)21)5-9(8)23-11-6-18-14(16)19-13(11)15/h4-7H,1-3H3,(H2,17,20,21)(H4,15,16,18,19)
InChi Key	HLWURFKMDLAKOD-UHFFFAOYSA-N
Canonical SMILES	CC(C)C1=CC(=C(C=C1OC2=CN=C(N=C2N)N)S(=O)(=O)N)OC
Isomeric SMILES	CC(C)C1=CC(=C(C=C1OC2=CN=C(N=C2N)N)S(=O)(=O)N)OC
Alternate CAS	1015787-98-0
PubChem CID	24764487
MeSH Entry Terms	5-((2,4-Diamino-5-pyrimidinyl)oxy)-4-isopropyl-2-methoxybenzenesulfonamide;AF-219;Benzenesulfonamide, 5-((2,4-diamino-5-pyrimidinyl)oxy)-2-methoxy-4-(1-methylethyl)-;Gefapixant;MK-7264
Molecular Weight	353.4

Certificates

Certificate of Analysis(COA)

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5 results found

Lot Number	Certificate Type	Date	Item
K2209587	Certificate of Analysis	Jul 28, 2022	G413575
K2209591	Certificate of Analysis	Jul 28, 2022	G413575
K2209592	Certificate of Analysis	Jul 28, 2022	G413575
K2209593	Certificate of Analysis	Jul 28, 2022	G413575
K2209594	Certificate of Analysis	Jul 28, 2022	G413575

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 71 mg/mL (200.9 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility	71
DMSO(mM) Max Solubility	200.905489530277
Water(mg / mL) Max Solubility	＜1

Safety and Hazards(GHS)

Pictogram(s)	GHS08, GHS07
Signal	Warning
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H373:Causes damage to organs through prolonged or repeated exposure H302:Harmful if swallowed
Precautionary Statements	P501:Dispose of contents/container to ... P260:Do not breathe dust/fume/gas/mist/vapors/spray. P319:Get medical help if you feel unwell.

References

1. Ford AP, Undem BJ. (2013) The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders.. Front Cell Neurosci, 7 (3): (267). [PMID:24391544]
2. Ochoa-Cortes F, Liñán-Rico A, Jacobson KA, Christofi FL. (2014) Potential for developing purinergic drugs for gastrointestinal diseases.. Inflamm Bowel Dis, 20 (7): (1259-87). [PMID:24859298]
3. Richards D, Gever JR, Ford AP, Fountain SJ. (2019) Action of MK-7264 (gefapixant) at human P2X3 and P2X2/3 receptors and in vivo efficacy in models of sensitisation.. Br J Pharmacol, 176 (13): (2279-2291). [PMID:30927255]
4. Markham A. (2022) Gefapixant: First Approval.. Drugs, 82 (6): (691-695). [PMID:35347635]

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