Home Metabolism Phospholipase (e.g. PLA) inhibitor Darapladib For research use only.

Darapladib

Synonyms: SB-480848

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

Darapladib Chemical Structure

Darapladib Chemical Structure

CAS: 356057-34-6

Selleck's Darapladib has been cited by 6 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Darapladib Related Products

Signaling Pathway

Phospholipase (e.g. PLA) Signaling Pathways

Phospholipase (e.g. PLA) Signaling Pathway

Choose Selective Phospholipase (e.g. PLA) Inhibitors

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-8-5-11 qHTS assay P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
KB-3-1 qHTS assay P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen 31515284
Click to View More Cell Line Experimental Data

Biological Activity

Description Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.
Targets
Lp-PLA2 [1]
(Cell-free assay)
0.25 nM
In vitro
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 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 Animal Models WHHL rabbits
Dosages ~30 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02000804 Completed
Atherosclerosis
GlaxoSmithKline
 October 23 2013 Phase 1
NCT01873339 Completed
Atherosclerosis
GlaxoSmithKline
 June 19 2013 Phase 1
NCT01852565 Completed
Atherosclerosis
GlaxoSmithKline
 May 14 2013 Phase 1
NCT01751074 Completed
Atherosclerosis
GlaxoSmithKline
 December 17 2012 Phase 1
NCT01711723 Completed
Atherosclerosis
GlaxoSmithKline
 October 29 2012 Phase 1
NCT01154114 Completed
Atherosclerosis
GlaxoSmithKline
 July 1 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 666.77 Formula

C36H38F4N4O2S
CAS No. 356057-34-6 SDF Download Darapladib SDF
Smiles CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (149.97 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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