2241651-99-8

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: 2024-01-12 13:24:51
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	Signaling Pathways >> Membrane Transporter/Ion Channel >> Sodium Channel Research Areas >> Neurological Disease
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