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MTK458

Catalog No.GC71210 Copy One-Click Copy Product Info

MTK458 is an orally active brain penetrant PINK1 activator.

Products are for research use only. Not for human use. We do not sell to patients.

MTK458 Chemical Structure

Cas No.: 2499962-58-0

Size Price Stock Qty
10mM (in 1mL DMSO)
$90.00
In stock
5 mg
$81.00
In stock
10 mg
$130.00
In stock
25 mg
$274.00
In stock
50 mg
$468.00
In stock
100 mg
$792.00
In stock

Tel:(909) 407-4943 Email: sales@glpbio.com


Customer Reviews

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Sample solution is provided at 25 µL, 10mM.



Description of MTK458

MTK458 is an orally active brain penetrant PINK1 activator. MTK458 binds to PINK1 and stabilizes an active heterocomplex, thereby increasing mitophagy. MTK458 can be used for research on Parkinson's disease.

MTK458 (25 µM) increases PINK1-mediated mitophagy to enhance clearance of intramitochondrial aggregates in Hela cells induced ΔOTC and YFP-Parkin[1].
MTK458 (0.1-25 µM) clears pS129 α-synuclein aggregates (12-250 kDa) in a dose-dependent manner in DIV9 and DIV12[1].
MTK458 (0-13 µM, 10 days) reduces α-synuclein pathology and the mitochondrial stress marker pUb in iPSC neurons[1].

MTK458 (50 mg/kg, p.o., daily, 6 months) drives clearance of pathologic α-synuclein in a dose-dependent manner in the stratum of mice injected with α-synuclein preformed fibrils (PFFs)[1].
MTK458 (50 mg/kg, p.o., 6 doses, 5 days) decreases plasma pS65-Ubiquitin (pUb) in wild-type Sprague-Dawley rats[1].

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.

Chemical Properties of MTK458

Cas No. 2499962-58-0 SDF
Formula C17H15F3N4 M.Wt 332.32
Solubility DMSO : 100 mg/mL (300.91 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Storage 4°C, sealed storage, away from moisture
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of MTK458

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.0091 mL 15.0457 mL 30.0915 mL
5 mM 601.8 μL 3.0091 mL 6.0183 mL
10 mM 300.9 μL 1.5046 mL 3.0091 mL
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In vivo Formulation Calculator (Clear solution) of MTK458

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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