1. Metabolic Enzyme/Protease
  2. Phospholipase

Darapladib (Synonyms: SB-480848)

Cat. No.: HY-10521 Purity: 99.95%
Handling Instructions

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

For research use only. We do not sell to patients.
Darapladib Chemical Structure

Darapladib Chemical Structure

CAS No. : 356057-34-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 220 In-stock
5 mg USD 150 In-stock
10 mg USD 276 In-stock
50 mg USD 1188 In-stock
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


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

IC50 & Target

IC50: 0.25 nM (Lp-PLA2)[1]

In Vitro

Mechanistic studies using steady state and transient kinetics indicate Darapladib (SB-480848) to be a freely reversible, non-covalently bound, inhibitor of rhLp-PLA2 with a Ki of 110 pM and an off-rate of 27 min. Potent inhibition of the enzyme in whole human plasma is confirmed (IC50=5±2 nM). Furthermore, the presence of Darapladib during the copper catalysed oxidation of human LDL prevents the production of lyso-PtdCho (IC50=4±3 nM) and subsequent monocyte chemotaxis (IC50=4±1 nM)[1].

In Vivo

Additional in vivo studies with Darapladib indicated an oral bioavailability of 11±2% in the fed rat. The oral bioavailability of Darapladib is 28±4% in the dog. Furthermore excellent inhibition of Lp-PLA2 within the atherosclerotic plaque is achieved for Darapladib, with 95±1% inhibition observed 2 h after an oral dose of 30 mg/kg to the WHHL rabbit[1]. Darapladib, a specific inhibitor of lipoprotein-associated phospholipase A2 (lp-PLA2), on inflammation and atherosclerotic formation in the low density lipoprotein receptor (LDLR)-deficient mice. the activity of serum lp-PLA2 is inhibited by more than 60% in LDLR-deficient mice after oral administration of 50 mg/kg once daily of Darapladib for 6 weeks. Darapladib significantly inhibits serum lp-PLA2 activity in LDLR-deficient mice[2].

Clinical Trial
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.4998 mL 7.4988 mL 14.9977 mL
5 mM 0.3000 mL 1.4998 mL 2.9995 mL
10 mM 0.1500 mL 0.7499 mL 1.4998 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration

Darapladib is prepared in saline (Mice)[2].

Male homozygous LDLR-deficient mice (C57/Bl6 genetic background) are fed a high-fat diet consisting of 18% hydrogenated cocoa butter, 0.15% cholesterol, 7% casein, 7% sucrose, and 3% maltodextrin for 17 weeks, beginning at 6 weeks of age. Forty mice are divided into two groups (n=20 per group) randomly. One group receive Darapladib by gavage (50 mg/kg per day) once daily, while the other group receive the vehicle (saline). During the 6 weeks of treatment, all mice are housed in a room with a 12-h light/dark cycle and are allowed free access to a high-fat diet and water. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight








Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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