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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 | Availability | Quantity |
---|---|---|---|
1 mg | $32 | In Stock | |
5 mg | $73 | In Stock | |
10 mg | Inquiry | 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]. |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (240.73 mM), Sonification is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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