SJ-300 is a potent and selective, orally active and brain-penetrat DKK3-LRP1 interaction inhibitor. SJ-300 restores Aβ clearance in AD models. SJ 300 binds to mLRPIV with a K d of 7.9 μM, inhibits the DKK3 mLRPIV complex with an IC 50 of 3.2 μM, and does not disrupt the binding of Aβ to LRP1 . SJ 300 rescues cognitive function and ameliorates neuropathology ( Aβ plaque reduction ≈ 73.3 %) in vivo. SJ 300 can be employed for research in Alzheimer’s disease.
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