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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.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $32 | - | In Stock | |
| 5 mg | $73 | In Stock | In Stock | |
| 10 mg | Preferential | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $80 | - | In Stock |
| 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), as a brain-penetrant small molecule, binds to PINK1 and stabilizes the active heterocomplex, thereby enhancing mitochondrial autophagy. It clears pS129 α-synuclein aggregates in a dose-dependent manner at DIV9 and DIV12[1]. |
| In vivo | In the striatum of mice injected with α-synuclein preformed fibrils (PFFs), Mitophagy activator 1 (50 mg/kg; oral gavage (p.o.), daily, for 6 months) rescued activity deficits in freely moving PFF mice and reduced the levels of inflammatory markers (TREM2, IL-6, and CXCL1)[1]. |
| Synonyms | Mitophagy activator 1, EP-0035985 |
| Molecular Weight | 332.32 |
| Formula | C17H15F3N4 |
| Cas No. | 2499962-58-0 |
| Smiles | N(C1=C2C(NC(C(F)(F)F)=C2)=NC=N1)[C@H]3C=4C(CCC3)=CC=CC4 |
| Storage | keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (240.73 mM), Sonification is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 3.3 mg/mL (9.93 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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