My cart
In the shopping cart is not goods, to choose and buy!
  • Product Name
  • Size
  • Quantity
  • Amount
    Selected items : 0 pieces Total : CHECK OUT()
    Darapladib (SB-480848)
    Darapladib (SB-480848)

    Market Price:

    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0844
    CAS #: 356057-34-6; Purity ≥98%

    Description: Darapladib (formerly also known as SB-480848; SB 480848; SB480848), a substituted pyrimidone, is a novel, potent and reversible inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with potential anti-inflammatory activity. It inhibits Lp-PLA2 with an IC50 of 0.25 nM. Darapladib is under development in Phase 3 clinical trials for the treatment of atherosclerosis.

    References: Bioorg Med Chem Lett. 2003;13(6):1067-70; Nat Med. 2008;14(10):1059-66; J Alzheimers Dis. 2013;35(1):179-98.

    Related CAS: 1389264-17-8 (Darapladib-impurity)

    Customer Validation
    Official Supplier of
    • VE
    • OF
    • YALE
    • hhmi
    • 香港大学
    Publications Citing InvivoChem Products
    • Physicochemical and Storage Information
    • Protocol
    • Quality Control Documentation
    • Related Biological Data
    • Customer Review
    Molecular Weight (MW)666.77
    CAS No.356057-34-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (150.0 mM)
    Water: <1 mg/mL
    Ethanol: 100 mg/mL (150.0 mM)
    Other infoChemical Name: N-[2-(diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-4,5,6,7-tetrahydro-4-oxo-N-[[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]-1H-Cyclopentapyrimidine-1-acetamide
    InChi Code: InChI=1S/C36H38F4N4O2S/c1-3-42(4-2)20-21-43(22-25-8-12-27(13-9-25)28-14-16-29(17-15-28)36(38,39)40)33(45)23-44-32-7-5-6-31(32)34(46)41-35(44)47-24-26-10-18-30(37)19-11-26/h8-19H,3-7,20-24H2,1-2H3
    SynonymsSB-480848; SB 480848; Darapladib; SB480848

    • Molarity Calculator
    • Dilution Calculator
    • The molarity calculator equation

      Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

      • Mass
      • Concentration
      • Volume
      • Molecular Weight *
      • =
      • ×
      • ×
    • The dilution calculator equation

      Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

      This equation is commonly abbreviated as: C1V1 = C2V2

      • Concentration (start)
      • ×
      • Volume (start)
      • =
      • Concentration (final)
      • ×
      • Volume (final)
      • ×
      • =
      • ×
      • C1
      • V1
      • C2
      • V2
    In Vitro

    In vitro activity:  During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM.

    Kinase Assay: Darapladib is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with IC50 of 0.25 nM.

    Cell Assay: Mechanistic studies using steady state and transient kinetics indicate Darapladib (SB-480848) to be a freely reversible, non-covalently bound, inhibitor of rhLp-PLA2 with a Ki of 110 pM and an off-rate of 27 min. Potent inhibition of the enzyme in whole human plasma is confirmed (IC50=5±2 nM). Furthermore, the presence of Darapladib during the copper catalysed oxidation of human LDL prevents the production of lyso-PtdCho (IC50=4±3 nM) and subsequent monocyte chemotaxis (IC50=4±1 nM). 

    In VivoIn the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. Darapladib, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. In DMHC pigs, darapladib reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons.
    Animal modelWHHL rabbits 
    Formulation & DosageDissolved in 1% aq methylcellulose; 30 mg/kg; p.o.
    ReferencesBioorg Med Chem Lett. 2003 Mar 24;13(6):1067-70; Nat Med. 2008 Oct;14(10):1059-66; J Alzheimers Dis. 2013;35(1):179-98.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Darapladib (SB-480848)

    Inhibition of Lp-PLA2 results in fewer lesion macrophages in coronary arteries. Nat Med. 2008 Oct;14(10):1059-66. 

    Darapladib (SB-480848)

    Inhibition of Lp-PLA2 results in fewer lesion macrophages in coronary arteries. Nat Med. 2008 Oct;14(10):1059-66.

    Darapladib (SB-480848)

    Influence of DM-HC induction and darapladib on arterial phospholipid composition. Nat Med. 2008 Oct;14(10):1059-66.


      Home Prev Next Last page / pices


      Your information is safe with us. * Required Fields.
      Products are for research use only;  We do not sell to patients
      Tel: 1-708-310-1919
      Fax: 1-708-557-7486
      Subscribe to our E-newsletter
      • Name*
      • *
      • E-mail*
      • *
      • instructions:
      • *
      Copyright 2020 InvivoChem LLC | All Rights Reserved
      Do you confirm the receipt?