Darapladib (SB-480848)

Catalog No.S7520

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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Darapladib (SB-480848) Chemical Structure

Darapladib (SB-480848) Chemical Structure
Molecular Weight: 666.77

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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]
IC50 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(Only for Reference)

Animal Study:


Animal Models WHHL rabbits
Formulation 1% aq methylcellulose
Dosages ~30 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Blackie JA, et al. Bioorg Med Chem Lett. 2003, 13(6), 1067-1070.

[2] Wilensky RL, et al. Nat Med. 2008, 14(10), 1059-1066.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
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

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Chemical Information

Download Darapladib (SB-480848) SDF
Molecular Weight (MW) 666.77


CAS No. 356057-34-6
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 100 mg/mL warming (149.97 mM)
Ethanol 100 mg/mL (149.97 mM)
Water <1 mg/mL
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 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

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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