MK-0557

CAS No. 328232-95-7

MK-0557( —— )

Catalog No. M24262 CAS No. 328232-95-7

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

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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2MG 74 In Stock
5MG 122 In Stock
10MG 186 In Stock
25MG 353 In Stock
50MG 530 In Stock
100MG 759 In Stock
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Biological Information

  • Product Name
    MK-0557
  • Note
    Research use only, not for human use.
  • Brief Description
    MK-0557 is a selective and orally available antagonist of the neuropeptide Y5 receptor (Ki: 1.6 nM).
  • 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.
  • 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.
  • Synonyms
    ——
  • Pathway
    GPCR/G Protein
  • Target
    Neuropeptide Y Receptor
  • Recptor
    neuropeptide Y (NPY) Y5 receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

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

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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