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MK-0354

CAS No. 851776-28-8

MK-0354( MK0354 )

Catalog No. M16190 CAS No. 851776-28-8

MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08 uM for hGPR109A and mGPR109A in the whole cell cAMP assays.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    MK-0354
  • Note
    Research use only, not for human use.
  • Brief Description
    MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08 uM for hGPR109A and mGPR109A in the whole cell cAMP assays.
  • Description
    MK-0354 is a potent, selective niacin receptor GPR109A partial agonist with EC50 of 1.65 and 1.08 uM for hGPR109A and mGPR109A in the whole cell cAMP assays; shows no interaction with any other target in a panel of over 120 other proteins; MK-0354 is a competitive inhibitor of 3H-nicotinic acid binding to hGPR109a with Ki of 505 nM, fully inhibits isoproterenol stimulated lipolysis in human adipocytes with IC50 of 3.1 uM, also is a competitive antagonist of nicotinic acid-induced MAPK signaling in cells overexpressing either mGPR109a or hGPR109a; possesses plasma FFA lowering effects in mice comparable to those of nicotinic acid, does not induce vasodilation.Atherosclerosis Phase 2 Discontinued.
  • In Vitro
    ——
  • In Vivo
    ——
  • Synonyms
    MK0354
  • Pathway
    GPCR/G Protein
  • Target
    GPR119
  • Recptor
    GPR119
  • Research Area
    Cardiovascular Disease
  • Indication
    Atherosclerosis

Chemical Information

  • CAS Number
    851776-28-8
  • Formula Weight
    176.1786
  • Molecular Formula
    C7H8N6
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 36 mg/mL
  • SMILES
    C12=C(CCC2)C(C3=NN=NN3)=NN1
  • Chemical Name
    Cyclopentapyrazole, 1,4,5,6-tetrahydro-3-(2H-tetrazol-5-yl)-

Shipping & Storage Information

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

Reference

1. Semple G, et al. J Med Chem. 2008 Aug 28;51(16):5101-8. 2. Lai E, et al. J Clin Lipidol. 2008 Oct;2(5):375-83. 3. Walters RW, et al. J Clin Invest. 2009 May;119(5):1312-21. 4. Gaidarov I, et al. Cell Signal. 2013 Oct;25(10):2003-16.
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