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Medchemexpress LLC AZ194 | 2241651-99-8 | 99.83% | C34H31F2N3O3 | 100 MG

Supplier: Medchemexpress LLC HY145169100MG
AZ194 is a first-in-class, orally active inhibitor of CRMP2-Ubc9 interaction and also acts as an inhibitor of NaV1.7, with an IC50 of 1.2 μM. It works by blocking the SUMOylation of CRMP2, which in turn selectively reduces the amount of surface-expressed NaV1.7. This compound demonstrates antinociceptive effects.
- Orally active inhibitor of CRMP2-Ubc9 interaction
- Acts as an inhibitor of NaV1.7 (IC50 of 1.2 μM)
- Blocks SUMOylation of CRMP2, reducing surface-expressed NaV1.7
- Demonstrates antinociceptive effects
- Provides pain relief in rat models of chemotherapy- and nerve injury-induced neuropathic pain
- Restores mechanical sensitivity when administered orally at 2 and 10 mg/kg
- Does not affect motor performance in male mice (10 mg/kg; ip; CD1)
- Synergizes with commonly used painkillers by engaging NaV1.7-dependent endogenous opioid signaling
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