PQ-912

Controlled Substances

Psychoactive Drugs/Narcotic Drugs/Hypertoxic Chemicals/Non-Medical Use of Narcotic Drugs and Psychotropic Substances

Names

[ Name ]:
PQ-912

Biological Activity

[Description]:

PQ-912 is a competitive inhibitor of the enzyme glutaminyl cyclase[1]. PQ-912 inhibits human, rat, and mouse glutaminyl cyclase activity, with Ki values ranging between 20 and 65 nM[2].

[Related Catalog]:

Signaling Pathways >> Others >> Others

Research Areas >> Neurological Disease

[Target]

Ki: 25 nM (human glutaminyl cyclase, pH:8.0); 65 nM (Mouse glutaminyl cyclase; pH:8.0)[2]

[In Vivo]

PQ-912 (oral treatment; 200 mg/kg/day for 1 week in hAPPSLxhQC double-transgenic mice) shows a significant reduction of pE-Aβ levels[2]. Animal Model: hAPPSLxhQC double-transgenic mice[2] Dosage: 200 mg/kg Administration: Oral treatment; daily for 1 week Result: Showed a significant reduction of pE-Aβ levels.

[References]

[1]. Lues I, et al. A phase 1 study to evaluate the safety and pharmacokinetics of PQ912, a glutaminyl cyclase inhibitor, in healthy subjects. Alzheimers Dement (N Y). 2015 Oct 3;1(3):182-195.

[2]. Hoffmann T, et al. Glutaminyl Cyclase Inhibitor PQ912 Improves Cognition in Mouse Models of Alzheimer's Disease-Studies on Relation to Effective Target Occupancy. J Pharmacol Exp Ther. 2017 Jul;362(1):119-130.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₉H₂₀N₄O₂

[ Molecular Weight ]:
336.39

[ Storage condition ]:
2-8°C

Safety Information

[ Hazard Codes ]:
Xn