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MTK458

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MTK458

Catalog No. T72420Cas No. 2499962-58-0

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.

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Pack Size	Price	Availability
1 mg	$93	In Stock
5 mg	$228	In Stock
10 mg	$363	In Stock
25 mg	$745	In Stock
50 mg	$1,180	In Stock
100 mg	$1,620	In Stock
1 mL x 10 mM (in DMSO)	$253	In Stock

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Product Introduction

Bioactivity

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

Chemical Properties

Molecular Weight	332.32
Formula	C17H15F3N4
Cas No.	2499962-58-0

Storage & Solubility Information

Storage

keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 80 mg/mL (240.73 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.0091 mL	15.0457 mL	30.0915 mL	150.4574 mL
5 mM	0.6018 mL	3.0091 mL	6.0183 mL	30.0915 mL
10 mM	0.3009 mL	1.5046 mL	3.0091 mL	15.0457 mL
20 mM	0.1505 mL	0.7523 mL	1.5046 mL	7.5229 mL
50 mM	0.0602 mL	0.3009 mL	0.6018 mL	3.0091 mL
100 mM	0.0301 mL	0.1505 mL	0.3009 mL	1.5046 mL

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A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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