Suzetrigine

SKU: orb1739928

Description

Suzetrigine (VX-548) is a selective, orally bioavailable inhibitor of the NaV1.8 sodium channel. It is a research tool for investigating acute pain mechanisms and neurotransmission, with applications in both in vitro electrophysiology studies and in vivo preclinical models of pain.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2649467-58-1
• MW: 473.39
• Purity: 99.76% (May vary between batches)
• Formula: C₂₁H₂₀F₅N₃O₄
• SMILES: C(NC=1C=C(C(N)=O)N=CC1)(=O)[C@H]2[C@@H]([C@H](C)[C@@]([C@@](F)(F)F)(C)O2)C3=C(OC)C(F)=C(F)C=C3
• Target: Sodium Channel
• Solubility: DMSO:161 mg/mL (340.1 mM)

Bioactivity

• Target IC50:
  NaV1.8 (mouse):210 nM|NaV1.8 (rat):56 nM|Nav1.8 (human):0.68 ± 0.16 nM|NaV1.8 (dog):740 nM|NaV1.8 (monkey):0.75 nM|NaV1.8 (rabbit):52 nM|NaV1.8:0.7 nM
• In Vivo:
  As compared with placebo, Suzetrigine at the highest dose (a 100-mg oral loading dose of Suzetrigine, followed by a 50-mg maintenance dose every 12 hours), but not at lower doses (a 20-mg loading dose, followed by a 10-mg maintenance dose every 12 hours), reduced acute pain over a period of 48 hours after abdominoplasty or bunionectomy.

Storage & Handling

• Storage: store at low temperature,keep away from direct sunlight | 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

Nav1.8 channel, Sodium Channel, SodiumChannel, Suzetrigine, VX 548, VX548, VX-548

Compound Identifiers

PubChem CID

156445116