Darapladib (SB-480848)

Catalog No.S7520

Darapladib (SB-480848) Chemical Structure

Molecular Weight(MW): 666.77

Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.

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Biological Activity

Description Darapladib (SB-480848) is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.
Lp-PLA2 [1]
(Cell-free assay)
0.25 nM
In vitro

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. [1]

In vivo In the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. [1] Darapladib, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. [2] In DMHC pigs, darapladib reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons. [3]


Animal Research:


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  • Animal Models: WHHL rabbits
  • Formulation: 1% aq methylcellulose
  • Dosages: ~30 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (149.97 mM)
Ethanol 100 mg/mL (149.97 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 666.77


CAS No. 356057-34-6
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01711723 Completed Atherosclerosis GlaxoSmithKline October 29 2012 Phase 1
NCT02058641 Completed Atherosclerosis GlaxoSmithKline February 26 2014 Phase 1
NCT00734032 Completed Atherosclerosis GlaxoSmithKline August 26 2008 Phase 2
NCT02000804 Completed Atherosclerosis GlaxoSmithKline October 23 2013 Phase 1
NCT01506895 Completed Retinopathy Diabetic GlaxoSmithKline February 2012 Phase 2
NCT01636271 Completed Coronary Heart Disease GlaxoSmithKline October 2011 --

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Phospholipase (e.g. PLA) Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID