Gefapixant

SKU: orb1227150

Description

Gefapixant (AF-219, MK-7264) is an orally active, small molecule antagonist of P2X3-containing receptor with IC50 of 30 nM (hP2X3 homotrimer) and 100-250 nM (hP2X2/3 heterotrimer); displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC50 >10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels); markedly and significantly reduced objective cough frequency in clinical trials.Asthma Phase 2 Clinical.

Key Properties

• CAS Number: 1015787-98-0
• MW: 353.397
• Purity: >98% (HPLC)
• Formula: C₁₄H₁₉N₅O₄S
• SMILES: O=S(C1=CC(OC2=CN=C(N)N=C2N)=C(C(C)C)C=C1OC)(N)=O
• Target: P2X Receptor
• Solubility: DMSO: 10 mM （(< 1 mg/ml )

Bioactivity

• In Vivo:
  Gefapixant (7d bid, orally) attenuates the weight bearing laterality with complete reversal of apparent hyperalgesia at the two higher doses in a rat model of knee osteoarthritis (14d following intra-articular administration of monoiodoacetate).
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• In Vitro:
  Gefapixant 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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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AF-219 | MK-7264

Quick Database Links

Gene Symbol

P2X Receptor