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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Eukaryotic Initiation Factor (eIF)-DNL343
DNL343

Chemical Structure : DNL343

CAS No.: 2278265-85-1

DNL343 (DNL-343, DNL 343)

货号: PC-22002Not For Human Use, Lab Use Only.

DNL343 is a potent, selective, and brain-penetrant eIF2B activator with IC50 of 3.2 nM in cellular ATF4 nano-Luciferase (nLuc) reporter assays.

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

生物&药学活性

DNL343 is a potent, selective, and brain-penetrant eIF2B activator with IC50 of 3.2 nM in cellular ATF4 nano-Luciferase (nLuc) reporter assays.
DNL343 is highly CNS-penetrant in a rat PK study with a brain-to-plasma unbound ratio (Bu/Pu) of 0.8.
Displays no activation of PXR, CAR, or AHR, as well as no significant effect against CEREP or kinase selectivity panels.
inhibits the formation of TDP43(86–414)-positive stress granules in a dose-dependent manner in H4 cells with IC50 of 13 nM.
DNL343 inhibits ISR activation in the brain of the Eif2b5 R191H knock-in mouse model, reduces ISR markers, shows potential therapeutic for the treatment of ALS.

物理化学性质&存储条件

分子量 457.83
分子式 C20H19ClF3N3O4
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

10 mM in DMSO

Chemical Name/SMILES

2-(4-Chlorophenoxy)-N-[3-[5-[cis-3-(trifluoromethoxy)cyclobutyl]-1,3,4-oxadiazol-2-yl]-1-bicyclo[1.1.1]pentanyl]acetamide

参考文献

1. Craig RA 2nd, et al. J Med Chem. 2024 Mar 21. doi: 10.1021/acs.jmedchem.3c02422.

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