AZ194
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].
Product Specifications
CAS Number
2241651-99-8
UNSPSC
12352005
Hazard Statement
H315, H319
Target
Sodium Channel
Type
Reference compound
Related Pathways
Membrane Transporter/Ion Channel
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/az194.html
Purity
99.83
Solubility
DMSO : 33.33 mg/mL (ultrasonic)
Smiles
O=C(N1CCC(CC1)C2=NC3=C(N2CC4=CC(F)=CC=C4)C=CC=C3)C5=CC=C(C(OC)=C5)OCC6=CC(F)=CC=C6
Molecular Formula
C34H31F2N3O3
Molecular Weight
567.63
Precautions
H315, H319
References & Citations
[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Nav1.7
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