MK-0557

Alias: MK-0557; MK 0557; MK0557

Cat No.:V4296 Purity: ≥98%

COA Product Data Instructions for use SDS

MK-0557 (MK0557) is a novel, highly selective, orally bioavailable neuropeptide Y5 receptor antagonist with anti-obesity effects.

MK-0557 Chemical Structure CAS No.: 328232-95-7
Product category: Neuropeptide Y Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

MK-0557 (MK0557) is a novel, highly selective, orally bioavailable neuropeptide Y5 receptor antagonist with anti-obesity effects. It inhibits neuropeptide Y5 receptor with a Ki of 1.6 nM. MK-0557 has the potential to treat obesity because it may prevent weight gain following weight loss that is brought about by a very-low-calorie diet (VLCD). Strongly orexigenic neuropeptide Y (NPY) is known, and antagonistic effects on NPY Y1 and NPY Y5 receptors (NPYxR) are thought to represent a promising therapeutic target for obesity prevention.

Biological Activity I Assay Protocols (From Reference)

Targets

NPY Y₅ receptor

ln Vitro

Neuropeptide Y (NPY) is a potent orexigenic neuropeptide, and antagonistic action on NPY Y1 and NPY Y5 receptors (NPYxR) is thought to represent a promising therapeutic target for obesity prevention. At the human NPY5R, MK-0557 exhibits a Ki=1.3 nM, while its affinities at the rhesus, mouse, and rat NPY5R are comparable. At concentrations of 10 μM, MK-0557 does not exhibit any significant binding to the human, mouse, or NPY1R, NPY2R, or NPY4R[2].

ln Vivo

MK-0557 significantly inhibits the body-weight gain in diet-induced obese (DIO) mice and counteracts the effects of the NPY5R-selective agonist on hyperphagia and body-weight gain in C57BL/6J mice. Day 35 body-weight gain is reduced by 40% when lean mice fed regular chow are given a medium high-fat diet (4.2 kcal/g) and administered MK-0557 at a dose of 30 mg/kg PO QD[2].

References

[1]. Discovery and evaluation of spirocyclic derivatives as antagonists of the neuropeptide Y5 receptor. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2738-43.

[2]. Neuropeptide Y5 receptor antagonism does not induce clinically meaningful weight loss in overweight and obese adults. Cell Metab. 2006 Oct;4(4):275-82.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C22H19FN4O3
Molecular Weight	406.4097
Exact Mass	406.14
Elemental Analysis	C, 65.02; H, 4.71; F, 4.67; N, 13.79; O, 11.81
CAS #	328232-95-7
Related CAS #	935765-76-7 (alternate)
Appearance	Solid powder
SMILES	C1CC2(CCC1C(=O)NC3=NN(C=C3)C4=CC=CC=C4F)C5=C(C=CN=C5)C(=O)O2
InChi Key	RMYZIRFUCOMQRH-UHFFFAOYSA-N
InChi Code	InChI=1S/C22H19FN4O3/c23-17-3-1-2-4-18(17)27-12-8-19(26-27)25-20(28)14-5-9-22(10-6-14)16-13-24-11-7-15(16)21(29)30-22/h1-4,7-8,11-14H,5-6,9-10H2,(H,25,26,28)
Chemical Name	N-[1-(2-fluorophenyl)pyrazol-3-yl]-1'-oxospiro[cyclohexane-4,3'-furo[3,4-c]pyridine]-1-carboxamide
Synonyms	MK-0557; MK 0557; MK0557
HS Tariff Code	2934.99.9001
Storage	Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)	DMSO: ~200 mg/mL (~492.1 mM) H2O: < 0.1 mg/mL
Solubility (In Vivo)	Solubility in Formulation 1: 5 mg/mL (12.30 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.)

Solubility (In Vitro)

DMSO: ~200 mg/mL (~492.1 mM)
H2O: < 0.1 mg/mL

Solubility (In Vivo)

Solubility in Formulation 1: 5 mg/mL (12.30 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	2.4606 mL	12.3028 mL	24.6057 mL
	5 mM	0.4921 mL	2.4606 mL	4.9211 mL
	10 mM	0.2461 mL	1.2303 mL	2.4606 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

Calculate Reset

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

Dosage mg/kg

Average weight of animals g

Dosing volume per animal μL

Number of animals

Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT00482430	Completed	Drug: MK0557 Drug: Comparator: Placebo (unspecified)	Schizophrenia Paranoid Schizophrenia	Merck Sharp & Dohme LLC	September 2007	Phase 2
NCT00533598	Completed	Drug: MK0557	Obesity	Merck Sharp & Dohme LLC	September 2002	Phase 2
NCT00092872	Completed	Drug: MK0557	Obesity	Merck Sharp & Dohme LLC	November 2003	Phase 3
NCT00092859	Completed	Drug: MK0557	Obesity	Merck Sharp & Dohme LLC	August 2003	Phase 3
NCT00533481	Completed	Drug: MK0557	Obesity	Merck Sharp & Dohme LLC	February 2004	Phase 2

Biological Data

Structures of MK-0557 and PET ligand [11C]MK-0233. Cell Metab . 2006 Oct;4(4):275-82.
Effects of MK-0557 on intracellular calcium and weight gain in mice. Cell Metab . 2006 Oct;4(4):275-82.