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
Size Price / USD Stock Quantity
1 mL x 10 mM in DMSO 69 In Stock
5MG 62 In Stock
10MG 93 In Stock
25MG 169 In Stock
50MG 272 In Stock
100MG 384 In Stock
200MG 535 In Stock
500MG Get Quote In Stock
1G Get Quote In Stock

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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