Bioactivity | ZJCK-6-46 (32) is a potential and orally activeDYRK1A inhibitor (IC50 = 0.68 nM) with high BBB permeability (CNS+). ZJCK-6-46 (32) reduces tau phosphorylation. ZJCK-6-46 (32) ameliorates cognitive dysfunction by obviously reducing the expression of phosphorylated tau and neuronal loss in vivo[1]. |
In Vivo | ZJCK-6-46 (32, 20-30 mg/kg, orally, OA-induced (MOD) mice) 显著下调OA (Okadaic acid, HY-N6785) 诱导小鼠的 CA1 区和 DG 区p-Tau thr212 的表达[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Formula | C24H21N5O |
Molar Mass | 395.46 |
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]. Huanhua Chen, et al. Discovery of ZJCK-6-46: A Potent, Selective, and Orally Available Dual-Specificity Tyrosine Phosphorylation-Regulated Kinase 1A Inhibitor for the Treatment of Alzheimer's Disease. J Med Chem. 2024 Aug 8;67(15):12571-12600. |