| Bioactivity | Glutaminyl Cyclase Inhibitor 5 (Compound 71) is a potent and selective human glutaminyl cyclase (hQC) inhibitor with an IC50 of 3.2 nM[1]. |
| Target | IC50: 3.2 nM (hQC), 34.2 nM (mQC), 106.1 nM (isoQC) |
| Invitro | Glutaminyl Cyclase Inhibitor 5 (Compound 71) 未表现出明显的 hERG 抑制 (10 μM 抑制率为 47.6%)[1]。Glutaminyl Cyclase Inhibitor 5 可能透过血脑屏障 (-log Pe = 5.5)[1]。 |
| In Vivo | Glutaminyl Cyclase Inhibitor 5 (Compound 71) (10 mM, 5 μL; ICV; once) 抑制急性阿尔茨海默病小鼠模型中 pE-Aβ3-40 形成,抑制率为 25%[1]。 Animal Model: |
| Name | Glutaminyl Cyclase Inhibitor 5 |
| Formula | C22H30N6O |
| Molar Mass | 394.51 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Van Manh N, et al. Discovery of potent indazole-based human glutaminyl cyclase (QC) inhibitors as Anti-Alzheimer's disease agents. Eur J Med Chem. 2022 Dec 15;244:114837. |