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.
Targets
Lp-PLA2 [1]
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]

Protocol

Animal Research:

[1]

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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 slightly soluble or insoluble
In vivo

* 1 mg/ml means slightly soluble or 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
Formula

C36H38F4N4O2S

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
NCT02058641 Completed Atherosclerosis GlaxoSmithKline February 2014 Phase 1
NCT02000804 Completed Atherosclerosis GlaxoSmithKline October 2013 Phase 1
NCT01873339 Completed Atherosclerosis GlaxoSmithKline June 2013 Phase 1
NCT01852565 Completed Atherosclerosis GlaxoSmithKline May 2013 Phase 1
NCT01751074 Completed Atherosclerosis GlaxoSmithKline December 2012 Phase 1
NCT01711723 Completed Atherosclerosis GlaxoSmithKline October 2012 Phase 1

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.

Handling Instructions

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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