1. GPCR/G Protein Neuronal Signaling
  2. Neuropeptide Y Receptor
  3. MK-0557

MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.

For research use only. We do not sell to patients.

MK-0557 Chemical Structure

MK-0557 Chemical Structure

CAS No. : 328232-95-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 149 In-stock
Solution
10 mM * 1 mL in DMSO USD 149 In-stock
Solid
5 mg USD 135 In-stock
10 mg USD 200 In-stock
50 mg USD 590 In-stock
100 mg USD 850 In-stock
200 mg USD 1160 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.

IC50 & Target

NPY Y5 receptor

 

In Vitro

Neuropeptide Y (NPY) is a potent orexigenic neuropeptide, and antagonism of NPY Y1 and NPY Y5 receptors (NPYxR) is considered a potentially important anti-obesity drug target. MK-0557 has a Ki=1.3 nM at the human NPY5R, with similar affinities at rhesus, mouse, and rat NPY5R. MK-0557 has no significant binding to the human NPY1R, NPY2R, NPY4R, or mouse NPY6R at concentrations of 10 μM[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

MK-0557 antagonizes the effects of the NPY5R-selective agonist on body-weight gain and hyperphagia in C57BL/6J mice and significantly suppresses the body-weight gain in diet-induced obese (DIO) mice. When lean mice on regular chow are switched to a medium high-fat diet (4.2 kcal/g) and treated with MK-0557 at 30 mg/kg PO QD, MK-0557 causes a 40% reduction in body-weight gain at day 35[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

406.41

Formula

C22H19FN4O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C([C@H]1CC[C@@](C2=C3C=CN=C2)(OC3=O)CC1)NC4=NN(C5=CC=CC=C5F)C=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (492.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: 5 mg/mL (12.30 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4606 mL 12.3028 mL 24.6057 mL 61.5142 mL
5 mM 0.4921 mL 2.4606 mL 4.9211 mL 12.3028 mL
10 mM 0.2461 mL 1.2303 mL 2.4606 mL 6.1514 mL
15 mM 0.1640 mL 0.8202 mL 1.6404 mL 4.1009 mL
20 mM 0.1230 mL 0.6151 mL 1.2303 mL 3.0757 mL
25 mM 0.0984 mL 0.4921 mL 0.9842 mL 2.4606 mL
30 mM 0.0820 mL 0.4101 mL 0.8202 mL 2.0505 mL
40 mM 0.0615 mL 0.3076 mL 0.6151 mL 1.5379 mL
50 mM 0.0492 mL 0.2461 mL 0.4921 mL 1.2303 mL
60 mM 0.0410 mL 0.2050 mL 0.4101 mL 1.0252 mL
80 mM 0.0308 mL 0.1538 mL 0.3076 mL 0.7689 mL
100 mM 0.0246 mL 0.1230 mL 0.2461 mL 0.6151 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
MK-0557
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HY-15411
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