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SAR439883

Chemical Structure : SAR439883

CAS No.:

SAR439883 (SAR 439883)

Catalog No.: PC-72066Not For Human Use, Lab Use Only.

SAR439883 (SAR 439883) is a novel potent, selective, orally active PKR inhibitor with IC50 of 0.68/0.69 uM against hPKR/mPKR, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SAR439883 (SAR 439883) is a novel potent, selective, orally active PKR inhibitor with IC50 of 0.68/0.69 uM against hPKR/mPKR, respectively.
SAR439883 dose-dependently ameliorated the AβO-induced cognitive impairment in both Y-maze and Morris Water Maze, prevented loss of synaptic proteins, and reduced levels of the proinflammatory cytokine interleukin-1β In both mouse models.
SAR439883 rescued memory deficits and prevented neurodegeneration in animal models of AD-like pathology, suggesting that inhibition of PKR is a potential therapeutic approach for AD.

Physicochemical Properties

M.Wt 384.852
Formula C19H23ClF2N2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-chloro-5-(((3R,5R,6R,8R)-3,6-difluoro-1-azaspiro[4.5]decan-8-yl)oxy)-3,3-dimethylisoindolin-1-one

References

1. Matilde Lopez-Grancha, et al. J Pharmacol Exp Ther. 2021 Sep;378(3):262-275.

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