Varoglutamstat (PQ912) is a potent glutaminyl cyclase (QC) inhibitor with Ki values of 20-65 nM for human, rat, and mouse QC activity.
Varoglutamstat (PQ912) shows fast association and dissociation kinetics with a KD value of 17 nM in SPR assays.
Varoglutamstat (PQ912) potently inhibits N3pE-Aβ40/42 formation in the APP-NLE/hQC model with EC50 of 0.14-0.25 uM.
Chronic oral treatment of hAPPSLxhQC double-transgenic mice with Varoglutamstat (PQ912) 200 mg/kg/day via chow shows a significant reduction of pE-Aβ levels and concomitant improvement of spatial learning in a Morris water maze test paradigm.
