Varoglutamstat (PQ912) | Glutaminyl cyclase inhibitor

Chemical Structure : PQ912

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PQ912 (Varoglutamstat, PQ 912)

货号: PC-21626Not For Human Use, Lab Use Only.

Varoglutamstat (PQ912) is a potent glutaminyl cyclase (QC) inhibitor with Ki values of 20-65 nM for human, rat, and mouse QC activity.

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生物&药学活性

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.

物理化学性质&存储条件

分子量	336.40
分子式	C19H20N4O2
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	(S)-1-(1H-benzo[d]imidazol-5-yl)-5-(4-propoxyphenyl)imidazolidin-2-one

参考文献

1. Zhang Y, et al. Eur J Pharmacol. 2022 Sep 15;931:175178.

2. Hoffmann T, et al. J Pharmacol Exp Ther. 2017 Jul;362(1):119-130.

PQ912 (Varoglutamstat, PQ 912)

生物&药学活性

物理化学性质&存储条件

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PQ912 (Varoglutamstat, PQ 912)

生物&药学活性

物理化学性质&存储条件

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