1276021-65-8

1276021-65-8 structure
1276021-65-8 structure
  • Name: PQ-912
  • Chemical Name: PQ-912
  • CAS Number: 1276021-65-8
  • Molecular Formula: C19H20N4O2
  • Molecular Weight: 336.39
  • Catalog: Research Areas Neurological Disease
  • Create Date: 2019-06-02 12:02:59
  • Modify Date: 2024-01-09 17:33:20
  • 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].

Name PQ-912
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
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.

Molecular Formula C19H20N4O2
Molecular Weight 336.39
Storage condition 2-8°C
Hazard Codes Xn