GX-585

SKU: orb1739565

Description

GX-585 is a sulfonamide-based small molecule inhibitor of the voltage-gated sodium channel Nav1.7. It exhibits analgesic properties and is utilized in preclinical research for investigating neuropathic pain and inflammatory pain mechanisms, both in vitro and in animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2098540-08-8
• MW: 539.45
• Purity: >99.99% (May vary between batches)
• Formula: C₂₄H₂₅Cl₂FN₄O₃S
• SMILES: CC=1C=2C(N(N1)[C@H]3CN([C@H](C)C4=CC(Cl)=CC(Cl)=C4)CC3)=CC(F)=C(C(NS(=O)(=O)C5CC5)=O)C2
• Target: Sodium Channel

Bioactivity

• Target IC50:
  Nav1.8:11.7μM
• In Vivo:
  METHODS: In an animal model of acute injury, the effects of once daily (q.d.) oral administration of 3 mg/kg and 10 mg/kg GX-585 were evaluated 2 hours after the first, fifth, or twelfth daily dose. RESULTS: A single 10 mg/kg dose of GX-585 produced analgesic effects similar to repeated 3 mg/kg doses 2 hours after administration, but the activity was completely reversed after 24 hours. Thus, the long-term effects of repeated dosing are inconsistent with slow losses of the compound from plasma.
• In Vitro:
  GX-585 is a potent inhibitor of NaV1.7 and highly selective for NaV1.5, but has different selectivity among neuronal NaV channels, with weaker inhibition of tetrodotoxin-resistant sodium currents in mouse DRG neurons, indicating weaker affinity for NaV1.8, with GX-585 blocking IC50 of 11.7 μM.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

MDK 3673, MDK-3673, GX585, GX-585, GX 585, Nav1.7 channel, Olfr895 Agonist 10, Olfr895 Agonist-10, Olfr895Agonist10, Olfr895-Agonist-10, Sodium Channel, SodiumChannel

Compound Identifiers

PubChem CID

129177689