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MRK-560

Name: MRK-560
Brand: TargetMol
SKU: T16133
Price: 35 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T16133Cas No. 677772-84-8

MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.

MRK-560

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Purity: 98.87%

Catalog No. T16133Cas No. 677772-84-8

MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$35	In Stock	In Stock
5 mg	$56	In Stock	In Stock
10 mg	$89	In Stock	In Stock
25 mg	$147	In Stock	In Stock
50 mg	$275	In Stock	In Stock
100 mg	$479	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$64	In Stock	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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Purity:98.87%

Appearance:Solid

Color:White

Resource Download

COA HNMR LCMS

Product Introduction

MRK-560 AI Summary

MRK-560 demonstrates significant bioactivity across various biological assays. Notably, it exhibits potent inhibition of gamma-secretase, reducing amyloid beta levels in multiple cell types including SHSY5Y neuroblastoma cells (IC50 = 0.65 nM), HEK293 cells (IC50 = 65.0 nM), and in HEK293 cells with specific IC50 values of 14.3 nM and 15.0 nM for amyloid beta 40 and 42, respectively. In vivo, the compound effectively lowers brain Abeta(40) levels in APP-YAC transgenic mice with a median effective dose (MED) of 1.0 mg/kg, and reduces Abeta42 production in an APP-Swedish transgenic mouse model at 10 mg/kg. Pharmacokinetically, MRK-560 demonstrates good oral bioavailability with an AUC of 1216.1 ng.hr.mL-1 in Sprague-Dawley rats at a 10 mg/kg dose, and reduces plasma amyloid beta levels by 71.0% in these rats after 3 hours. The compound also shows antiviral properties, inhibiting SARS-CoV-2 induced cytotoxicity in Caco-2 and VERO-6 cells at a 10 µM concentration with inhibition rates of 11.23% and 0.51%, respectively, and exhibits 3.759% inhibition of SARS-CoV-2 3CL-Pro protease at 20 µM. Moreover, MRK-560 interacts with multiple proteins, affecting their stability in Thermal Shift Assays and demonstrating a strong bioactive profile in phenotypic assays. It also shows selectivity in its enzymatic inhibition profile, with moderate activity against CYP3A4 and negligible or very weak inhibition against CYP2D6 and CYP2C9..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description

MRK-560 is an effective and brain-penetrant inhibitor of γ-secretase.

Chemical Properties

Molecular Weight	517.92
Formula	C₁₉H₁₇ClF₅NO₄S₂
Cas No.	677772-84-8
Smiles	Fc1ccc(F)c(c1)[C@]1(CC[C@@H](CC1)NS(=O)(=O)C(F)(F)F)S(=O)(=O)c1ccc(Cl)cc1
Relative Density.	1.57 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 60 mg/mL (115.85 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.86 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	1.9308 mL	9.6540 mL	19.3080 mL	96.5400 mL
5 mM	0.3862 mL	1.9308 mL	3.8616 mL	19.3080 mL
10 mM	0.1931 mL	0.9654 mL	1.9308 mL	9.6540 mL
20 mM	0.0965 mL	0.4827 mL	0.9654 mL	4.8270 mL
50 mM	0.0386 mL	0.1931 mL	0.3862 mL	1.9308 mL
100 mM	0.0193 mL	0.0965 mL	0.1931 mL	0.9654 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