Darapladib (SB-480848)

Catalog No.S7520

For research use only.

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

Darapladib (SB-480848) Chemical Structure

CAS No. 356057-34-6

Selleck's Darapladib (SB-480848) has been cited by 3 Publications

Purity & Quality Control

Choose Selective Phospholipase (e.g. PLA) Inhibitors

Other Phospholipase (e.g. PLA) Products

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]
(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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KB-8-5-11 MUjxTHRUKGG|c3H5 M3TQOXAu\2y7Y3;wdo91\WmwIIP1ZpN1emG2ZYOgbYRmdnSrZnnl[EBqdiCNQj24MVUuOTFiYXTlco9k[XKlaX7vcYEh[2WubDDsbY5mNCCzSGTTJJRp\XKjcHX1eIlkKGyrYoLhdpkhe2O{ZXXu MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTVzNUK4OEc,OzF3MUWyPFQ9N2F-
KB-3-1 MkTNdWhVWyCjc4PhfS=> MUPQMYdtgWOxcILveIVqdiC|dXLzeJJifGW|IHnk[Y51cW[rZXSgbY4hU0JvMz2xJIFl\W6xY3HyZ4lvd22jIHPlcIwhdGmwZTygdWhVWyC2aHXyZZBmfXSrYzDsbYJz[XK7IIPjdoVmdg>? M2XF[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNzNUG1Nlg1Lz5|MUWxOVI5PDxxYU6=
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 (from reference)

Animal Research:

[1]

  • Animal Models: WHHL rabbits
  • Dosages: ~30 mg/kg
  • Administration: p.o.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 666.77
Formula

C36H38F4N4O2S

CAS No. 356057-34-6
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02000804 Completed Drug: darapladib 160mg Atherosclerosis GlaxoSmithKline October 23 2013 Phase 1
NCT01873339 Completed Drug: Darapladib|Drug: Midazolam Atherosclerosis GlaxoSmithKline June 19 2013 Phase 1
NCT01852565 Completed Drug: Darapladib|Drug: Diltiazem Atherosclerosis GlaxoSmithKline May 14 2013 Phase 1
NCT01751074 Completed Drug: Rosuvastatin 10 mg|Drug: Darapladib 160 mg Atherosclerosis GlaxoSmithKline December 17 2012 Phase 1
NCT01711723 Completed Drug: Darapladib 160 mg Atherosclerosis GlaxoSmithKline October 29 2012 Phase 1
NCT01154114 Completed Drug: darapladib Atherosclerosis GlaxoSmithKline July 1 2010 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Darapladib (SB-480848) | Darapladib (SB-480848) supplier | purchase Darapladib (SB-480848) | Darapladib (SB-480848) cost | Darapladib (SB-480848) manufacturer | order Darapladib (SB-480848) | Darapladib (SB-480848) distributor