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Gefapixant

Catalog No. T5099 CAS 1015787-98-0

Synonyms: RO 4926219, AF219, MK-7264

Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.

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Gefapixant, CAS 1015787-98-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 38.00
2 mg	In stock	$ 54.00
5 mg	In stock	$ 89.00
10 mg	In stock	$ 128.00
25 mg	In stock	$ 263.00
50 mg	In stock	$ 425.00
100 mg	In stock	$ 628.00
1 mL * 10 mM (in DMSO)	In stock	$ 98.00

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Purity: 99.26%

Biological Description

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Description	Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors.
Targets&IC50	P2X2/3 heterotrimeric receptors (human):100-250 nM, Recombinant hP2X3 homotrimers:~30 nM
In vitro	The IC50 of Gefapixant has been reported as ~30 nM versus recombinant hP2X3 homotrimers and 100-250 nM at hP2X2/3 heterotrimeric receptors, potencies very similar to those reported for recombinant rat receptors, and it displays no inhibitory impact on any non-P2X3 subunit-containing receptors (IC50 values>>10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5, and hP2X7 channels).
In vivo	In a rat model for knee osteoarthritis (developed 14 days after the intra-articular injection of monoiodoacetate), oral administration of Gefapixant twice daily for seven days resulted in a significant attenuation of weight bearing asymmetry, with a full reversal of observable hyperalgesia at the two higher doses [2].
Animal Research	A rodent model often employs for assessing the potential for drug effect in osteoarthritis (OA) pain is based on the intraarticular injection of monoiodoacetate (mIOA) into one knee joint of the rat. To measure the effect of Gefapixant on the weight bearing laterality and apparent hyperalgesia, Gefapixant is given by intraplantar or oral administration to the rats, with different concentrations (6, 20, and 60 mg/kg) two times a day and continues up to a week[2].

Synonyms	RO 4926219, AF219, MK-7264
Molecular Weight	353.4
Formula	C14H19N5O4S
CAS No.	1015787-98-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: < 10 mM(< means unknown)

H2O: Insoluble

References and Literature

1. Anthony P. Ford, et al. The therapeutic promise of ATP antagonism at P2X3 receptors in respiratory and urological disorders. Front Cell Neurosci. 2013; 7: 267. 2. Ford AP, In pursuit of P2X3 antagonists: novel therapeutics for chronic pain and afferent sensitization. Purinergic Signal. 2012 Feb;8(Suppl 1):3-26.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Gefapixant 1015787-98-0 Membrane transporter/Ion channel Neuroscience P2X Receptor RO4926219 AF-219 RO 4926219 AF219 inhibit chronic cough MK 7264 AF 219 MK-7264 P2X3 knee osteoarthritis Inhibitor RO-4926219 MK7264 P2XRs inhibitor

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