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AZ194

  Cat. No.:  DC60184   Featured
Chemical Structure
2241651-99-8
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More than 5000 active chemicals with high quality for research!
Field of application
AZ-194 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].
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2241651-99-8
Chemical Name: (4-(1-(3-Fluorobenzyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)(4-(3-fluorobenzyloxy)-3-methoxyphenyl)methanone
Synonyms: CRMP2-Ubc9-NaV1.7 inhibitor; HUN51998; HUN-51998; HUN 51998;
SMILES: O=C(N1CCC(C2=NC3=CC=CC=C3N2CC4=CC=CC(F)=C4)CC1)C5=CC=C(OCC6=CC=CC(F)=C6)C(OC)=C5
Formula: C34H31F2N3O3
M.Wt: 567.64
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: [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.
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].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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