AZ194 (CRMP2-Ubc9 inhibitor 194) is a potent and selective inhibitor of NaV1.7 currents in DRG neurons via inhibition of the CRMP2-Ubc9 interaction.
Compound 194 exhibited selective in vitro and ex vivo NaV1.7 engagement.
Orally administered 194 was not only antinociceptive in preclinical models of acute and chronic pain but also demonstrated synergy alongside other analgesics-without eliciting addiction, rewarding properties, or neurotoxicity.
Compound 19 is a first-in-class protein-protein inhibitor that capitalizes on CRMP2-NaV1.7 regulation to deliver safe analgesia in rodents.
Compound 194 is a robust inhibitor of chemotherapy induced peripheral neuropathy (CIPN) that reduces established neuropathic pain and prevents the emergence of neuropathic pain during treatment with multiple anti-neoplastic agents in both mice and rats.
