Gefapixant citrate

SKU: orb1686191

Description

Gefapixant citrate

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2310299-91-1
• MW: 545.52
• Purity: 99.98% (May vary between batches)
• Formula: C₂₀H₂₇N₅O₁₁S
• SMILES: O=C(O)CC(O)(C(=O)O)CC(=O)O.O=S(=O)(N)C=1C=C(OC2=CN=C(N=C2N)N)C(=CC1OC)C(C)C
• Target: P2X Receptor
• Solubility: DMSO:4 mg/mL (7.33 mM)

Bioactivity

• In Vivo:
  In a rat model of knee osteoarthritis, Gefapixant citrate (administered orally twice daily for 7 days) was able to attenuate the abnormal response on the weight-loading side and completely reversed the significant nociceptive hypersensitivity at the two higher doses (20 mg/kg and 60 mg/kg) (the model was established by intra-articular injections of monoiodoacetic acid and was observed for 14 days post-injection).
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• In Vitro:
  Gefapixant citrate did not inhibit any receptor that did not contain a P2X3 subunit, and its IC50 values exceeded 10,000 nM on recombinant hP2X1, hP2X2, hP2X4, rP2X5, and hP2X7 channels.
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Storage & Handling

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

Alternative Names

AF219 citrate, AF-219 citrate, MK7264 citrate, MK-7264 citrate, P2XReceptor, P2X Receptor, P2X3, RO4926219 citrate, RO 4926219 citrate

Compound Identifiers

PubChem CID

145720531