MK-0557

SKU: orb1218162

Description

MK-0557 is a selective and orally available antagonist of the neuropeptide Y5 receptor (Ki: 1.6 nM).(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.(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.

Key Properties

• CAS Number: 328232-95-7
• MW: 406.41
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₈FN₄O₃
• SMILES: O=C([C@H]1CC[C@@](C2=C3C=CN=C2)(OC3=O)CC1)NC4=NN(C5=CC=CC=C5F)C=C4
• Target: Neuropeptide Y Receptor
• Solubility: DMSO:25 mg/mL (61.52 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Neuropeptide Y Receptor