| Description | MTK458 (EP-0035985) is an orally active and brain-permeable PINK1 activator that promotes pathological clearance of alpha-synuclein and reduces pUb in a PFF inoculation model.MTK458 induces pathological alpha-synuclein clearance by stimulating dimerization and stabilization of the PINK1/TOM complex.MTK458 may be used in Parkinson's disease research. |
| In vitro | Mitophagy activator 1(0.1-25 µM) 作为脑渗透性小分子，可与PINK1结合并稳定活性异质复合物，从而增加线粒体自噬，在 DIV9 和 DIV12 中以剂量依赖的方式清除 pS129 α-突触核蛋白聚集体[1]。 |
| In vivo | 在注射了 α-突触核蛋白预形成纤维（PFFs）的小鼠的基底部位中，Mitophagy activator 1（50 mg/kg；口服灌胃（p.o.），每日一次，6个月）能够挽救自由活动的 PFF 小鼠的活动缺陷，并降低炎症标志物（TREM2、IL-6 和 CXCL1）的水平[1]。 |
| Synonyms | Mitophagy activator 1, EP-0035985 |
| molecular weight | 332.32 |
| Molecular formula | C17H15F3N4 |
| CAS | 2499962-58-0 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80 mg/mL (240.73 mM), Sonification is recommended. |
| References | 1. Chin RM, et al. Pharmacological PINK1 activation ameliorates Pathology in Parkinson's Disease models. bioRxiv [Preprint]. 2023 Feb 15:2023.02.14.528378. |