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2241651-99-8

2241651-99-8 structure
2241651-99-8 structure
  • Name: AZ194
  • Chemical Name: CRMP2-Ubc9-NaV1.7 inhibitor 194
  • CAS Number: 2241651-99-8
  • Molecular Formula: C34H31F2N3O3
  • Molecular Weight: 567.62
  • Catalog: Signaling Pathways Membrane Transporter/Ion Channel Sodium Channel
  • Create Date: 2022-03-25 10:04:04
  • Modify Date: 2025-08-27 12:58:29
  • AZ194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and inhibitor of NaV1.7 (IC50=1.2 μM). AZ194 blocks SUMOylation of CRMP2 to selectively reduce the amount of surface-expressed NaV1.7. Antinociceptive effects[1].

Name CRMP2-Ubc9-NaV1.7 inhibitor 194
Description AZ194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and inhibitor of NaV1.7 (IC50=1.2 μM). AZ194 blocks SUMOylation of CRMP2 to selectively reduce the amount of surface-expressed NaV1.7. Antinociceptive effects[1].
Related Catalog
In Vivo AZ194 would provide pain relief in rat models of chemotherapy- and nerve injury- induced neuropathic pain. AZ194 (orally; at 2 and 10 mg/kg) restores mechanical sensitivity in animals with chemotherapy-induced and nerve injury-induced neuropathic nociception[1]. AZ194 (10 mg/kg; ip; CD1 male mice) does not affect motor performance (open field). AZ194 synergizes with commonly used painkillers, engages NaV1.7-dependent endogenous opioid signaling[1].
References

[1]. Cai S, et al. Selective targeting of NaV1.7 via inhibition of the CRMP2-Ubc9 interaction reduces pain in rodents. Sci Transl Med. 2021;13(619):eabh1314.

Molecular Formula C34H31F2N3O3
Molecular Weight 567.62
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