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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Sodium Channel-AZ194
AZ194

Chemical Structure : AZ194

CAS No.: 2241651-99-8

AZ194 (CRMP2-Ubc9 inhibitor 194)

货号: PC-72811Not For Human Use, Lab Use Only.

AZ194 (CRMP2-Ubc9 inhibitor 194) is a potent and selective inhibitor of NaV1.7 currents in DRG neurons via inhibition of the CRMP2-Ubc9 interaction.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

AZ194 (CRMP2-Ubc9 inhibitor 194) is a potent and selective inhibitor of NaV1.7 currents in DRG neurons via inhibition of the CRMP2-Ubc9 interaction.
Compound 194 exhibited selective in vitro and ex vivo NaV1.7 engagement.
Orally administered 194 was not only antinociceptive in preclinical models of acute and chronic pain but also demonstrated synergy alongside other analgesics-without eliciting addiction, rewarding properties, or neurotoxicity.
Compound 19 is a first-in-class protein-protein inhibitor that capitalizes on CRMP2-NaV1.7 regulation to deliver safe analgesia in rodents.
Compound 194 is a robust inhibitor of chemotherapy induced peripheral neuropathy (CIPN) that reduces established neuropathic pain and prevents the emergence of neuropathic pain during treatment with multiple anti-neoplastic agents in both mice and rats.

物理化学性质&存储条件

分子量 567.637
分子式 C34H31F2N3O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

50 mM in DMSO (28.5 mg/mL)

Chemical Name/SMILES

(4-(1-(3-Fluorobenzyl)-1H-benzo[d]imidazol-2-yl)piperidin-1-yl)(4-((3-fluorobenzyl)oxy)-3-methoxyphenyl)methanone

参考文献

1. Kathryn Braden, et al. Neurobiol Pain. 2021 Dec 27;11:100082.

2. Song Cai, et al. Sci Transl Med. 2021 Nov 10;13(619):eabh1314.

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