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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 |
| 2MG | 74 | In Stock |
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| 5MG | 122 | In Stock |
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| 10MG | 186 | In Stock |
|
| 25MG | 353 | In Stock |
|
| 50MG | 530 | In Stock |
|
| 100MG | 759 | In Stock |
|
| 200MG | 1044 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameMK-0557
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NoteResearch use only, not for human use.
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Brief DescriptionMK-0557 is a selective and orally available antagonist of the neuropeptide Y5 receptor (Ki: 1.6 nM).
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DescriptionMK-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.
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In VitroNeuropeptide 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.
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In VivoMK-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.
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Synonyms——
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PathwayGPCR/G Protein
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TargetNeuropeptide Y Receptor
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Recptorneuropeptide Y (NPY) Y5 receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number328232-95-7
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Formula Weight406.41
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Molecular FormulaC22H18FN4O3
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Purity>98% (HPLC)
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SolubilityDMSO:25 mg/mL (61.52 mM)
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SMILESO=C([C@H]1CC[C@@](C2=C3C=CN=C2)(OC3=O)CC1)NC4=NN(C5=CC=CC=C5F)C=C4
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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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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