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

MK-0557 

Cat. No.: HY-15411 Purity: 99.76%
Handling Instructions

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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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 185 In-stock
Estimated Time of Arrival: December 31
5 mg USD 168 In-stock
Estimated Time of Arrival: December 31
10 mg USD 264 In-stock
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50 mg USD 792 In-stock
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100 mg USD 1320 In-stock
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200 mg USD 1920 In-stock
Estimated Time of Arrival: December 31
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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

Ki: 1.6 nM (Y5)[1]

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].

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].

Clinical Trial
Molecular Weight

406.41

Formula

C₂₂H₁₉FN₄O₃

CAS No.

328232-95-7

SMILES

O=C([[email protected]]1CC[[email protected]@](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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 28 mg/mL (68.90 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2461 mL 1.2303 mL 2.4606 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

MK-0557MK0557MK 0557Neuropeptide Y ReceptorNPY receptorInhibitorinhibitorinhibit

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MK-0557
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HY-15411
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