AZ194是一流的口服活性 CRMP2-Ubc9 相互作用抑制剂和 NaV1.7 抑制剂 (IC50=1.2 μM)。AZ194 阻断 CRMP2 的 SUMOylation 以选择性地减少表面表达 NaV1.7 的量。具有抗伤害作用。
货号:ajcx36386
CAS:2241651-99-8
分子式:C34H31F2N3O3
分子量：567.63
溶解度:DMSO : 33.33 mg/mL (58.72 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

[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.