Desription: CRMP2-Ubc9-NaV1.7 inhibitor 194 can prevent the SUMOylation of the NaV1.7-interacting protein CRMP2 and reduce NaV1.7 surface expression as well as current density. CRMP2-Ubc9-NaV1.7 inhibitor 194 showed high selectivity for NaV1.7 and reduced acute and chronic pain in rodent models, after oral administration, without triggering adverse events. The results suggest that targeting posttranslational mechanisms might be an effective approach to selectively block NaV1.7 and obtain antinociceptive effects. Vvoltage-gated sodium channel 1.7 (NaV1.7) as one of the most promising targets for treating acute and chronic pain. However, the lack of selectivity of current NaV1.7 channel blockers hindered the development of effective treatments.

References: DOI: 10.1126/scitranslmed.abh1314

纯度：≥98%

CAS：2241651-99-8