Gefapixant

SKU: orb1302092

Description

Gefapixant (AF219) is a selective P2X3 receptor antagonist, exhibiting IC50 values of approximately 30 nM at human P2X3 homotrimers and 100-250 nM at P2X2/3 heterotrimers. This investigational compound is widely used in preclinical in vitro and in vivo research for studying purinergic signaling, chronic cough mechanisms, and airway hypersensitivity.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1015787-98-0
• MW: 353.4
• Purity: 99.72% (May vary between batches)
• Formula: C₁₄H₁₉N₅O₄S
• SMILES: COc1cc(C(C)C)c(Oc2cnc(N)nc2N)cc1S(N)(=O)=O
• Target: P2X Receptor
• Solubility: H2O:Insoluble;DMSO:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  P2X2/3 heterotrimeric receptors (human):100-250 nM|Recombinant hP2X3 homotrimers:~30 nM
• 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 .
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• 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).
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RO4926219, RO-4926219, RO 4926219, P2XRs, P2XReceptor, P2X3, P2X Receptor, Inhibitor, Gefapixant, MK 7264, MK7264, MK-7264, knee osteoarthritis, inhibit, chronic cough, AF219, AF-219, AF 219

Compound Identifiers

PubChem CID

24764487