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MTK458

Name: MTK458
Brand: TargetMol
SKU: T72420
Price: 80 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T72420Cas No. 2499962-58-0

Alias Mitophagy activator 1, EP-0035985

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.

MTK458

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Purity: 98.36%

Catalog No. T72420Alias Mitophagy activator 1, EP-0035985Cas No. 2499962-58-0

Pack Size	Price	USA Warehouse	Global Warehouse
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

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:98.36%

Appearance:Solid

Color:White

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COA HPLC HNMR

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].
Synonyms	Mitophagy activator 1, EP-0035985

Chemical Properties

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 & Solubility Information

Storage

keep away from moisture | 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 recommended.

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

	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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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc