Darapladib
Based on 8 publication(s) in Google Scholar
Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer.
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- Pureza: 99.92%
- No. CAS: 356057-34-6
- Fòrmula: C36H38F4N4O2S
- Peso molecular:666.77
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Darapladib
More- Autophagy. 2026 Mar 5. [Abstract]
- J Med Chem. 2016 May 26;59(10):5115-20. [Abstract]
- Inflamm Res. 2026 Apr 28;75(1):105. [Abstract]
- RSC Adv. 2017, 7(83):52762-52771.
- Eur J Pharmacol. 2020 Nov 15;887:173559. [Abstract]
- J Lipid Res. 2025 Jan 6:100742. [Abstract]
- Sci Rep. 2017 Oct 3;7(1):12628. [Abstract]
- Università Vita-Salute San Raffaele. 2022 Apr 08. 34.
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Ver todos los productos específicos de isoformas Phospholipase
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Actividad biológica
IC50: 0.25 nM (Lp-PLA2)[1]
Darapladib (5 μM; 6, 12 h) induces cell cycle arrest in glioma cells (C6 glioma cells and U251MG cells)[2].
Darapladib (5 μM; 3, 6 h) triggers cell apoptosis in glioma cells[2].
Darapladib (5 μM; 5, 15, 30, 60 and 90 min) induces an increase in phosphorylation of ERK1/2 proteins in glioma cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:C6 glioma cells and U251MG cells.
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Concentration:5 μM
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Incubation Time:3, 6 h
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Result:Triggered cell apoptosis in glioma cells.
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Cell Line:C6 glioma cells and U251MG cells.
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Concentration:5 μM
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Incubation Time:6, 12 h
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Result:Induced cell cycle arrest in glioma cells.
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Cell Line:C6 glioma cells and U251MG cells.
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Concentration:5 μM
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Incubation Time:5, 15, 30, 60 and 90 min
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Result:Induced an increase in phosphorylation of ERK1/2 proteins, but reduced AKT phosphorylation in glioma cells.
Darapladib (50 mg/kg; p.o.; once daily for 6 weeks) decreases serum hs-CRP and IL-6 levels[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male homozygous LDLR-deficient mice (C57/Bl6 genetic background)[3].
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Dosage:50 mg/kg
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Administration:Oral administration; once daily for 6 weeks.
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Result:Significantly inhibited activity of serum Lp-PLA2.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 356057-34-6
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Appearance Solid
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Peso molecular 666.77
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Fòrmula C36H38F4N4O2S
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Color White to off-white
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SMILES
FC1=CC=C(CSC(N(CC(N(CCN(CC)CC)CC2=CC=C(C3=CC=C(C(F)(F)F)C=C3)C=C2)=O)C4=C5CCC4)=NC5=O)C=C1
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Synonyms
SB-480848
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Autophagy
2026 Mar 5. PMID: 41787744 -
J Med Chem
Structural and Thermodynamic Characterization of Protein-Ligand Interactions Formed between Lipoprotein-Associated Phospholipase A2 and Inhibitors. [Abstract]2016 May 26;59(10):5115-20. PMID: 27078579 -
Inflamm Res
Lp-PLA2-derived LysoPC drives dendritic cell immunogenic activation and Th17 inflammation in severe asthma. [Abstract]2026 Apr 28;75(1):105. PMID: 42049997 -
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Eur J Pharmacol
Urocortin participates in LPS-induced apoptosis of THP-1 macrophages via S1P-cPLA2 signaling pathway. [Abstract]2020 Nov 15;887:173559. PMID: 32949605 -
J Lipid Res
Contribution of individual phospholipase A2 enzymes to the cleavage of oxidized phospholipids in human blood plasma. [Abstract]2025 Jan 6:100742. PMID: 39778770
Darapladib purchased from MedChemExpress. Usage Cited in: J Lipid Res. 2025 Jan 6:100742. [Abstract]
Incubation with 1:100 diluted pooled human plasma and Darapladib (10 nM) was performed for 90 min. Note that degradation of highly oxygenated full-length species was faster and less sensitive to darapladib inhibition.
Darapladib purchased from MedChemExpress. Usage Cited in: J Lipid Res. 2025 Jan 6:100742. [Abstract]
Darapladib but not other PLA2 inhibitors strongly reduces generation of LysoPC 16:0 and LysoPE 16:0 from oxidized precursors.
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Sci Rep
Maternal Gestational Diabetes Mellitus increases placental and foetal lipoprotein-associated Phospholipase A2 which might exert protective functions against oxidative stress. [Abstract]2017 Oct 3;7(1):12628. PMID: 28974763
Darapladib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Oct 3;7(1):12628. [Abstract]
LpPLA2 activity is abolished by addition of 150 nM Darapladib (24-120 h), a specific LpPLA2-inhibitor.
Darapladib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Oct 3;7(1):12628. [Abstract]
Anti-oxidative potential of HDL-LpPLA2 on neonatal placental endothelium. (a) Barrier function assay of placental endothelial cells exposed to (i) oxidized phospholipid mix (oxPL, 15 ug/ml, green), (ii) oxPL plus neonatal HDL (15 μg/ml + 200 μg/ml, dark blue) and (iii) oxPL plus neonatal HDL in the presence of Darapladip (15 ug/ml + 200 ug/ml + 150 nM, resp.; turquoise). Darapladib alone (light blue) did not show any off-target effects compared to endothelial basal medium (EBM, red). One out of five representative experiments is shown. *p < 0.05 compared to EBM, †p < 0.005 compared to oxPL.
Darapladib purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Oct 3;7(1):12628. [Abstract]
Cell free assay of Control HDL (black) and GDM- HDL (grey) anti-oxidative potential based on the oxidation of 123-dihydrorhodamine (DHR). In addition to LpPLA2-inhibition by Darapladib, also Paraoxanase-1 (PON-1) was inhibited by 2-hydroxyquinolone (2-OHQ). One-way ANOVA was used to test for significance.
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Solvente y solubilidad
DMSO : ≥ 100 mg/mL (149.98 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.75 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Blackie JA, et al. The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg Med Chem Lett. 2003 Mar 24;13(6):1067-70. [Content Brief]
[2]. Wang YJ, et al. The selective lipoprotein-associated phospholipase A2 inhibitor darapladib triggers irreversible actions on glioma cell apoptosis and mitochondrial dysfunction. Toxicol Appl Pharmacol. 2020 Sep 1;402:115133. [Content Brief]
[3]. Hu MM, et al. The inhibition of lipoprotein-associated phospholipase A2 exerts beneficial effects against atherosclerosis inLDLR-deficient mice. Acta Pharmacol Sin. 2011 Oct;32(10):1253-1258. [Content Brief]
[4]. Riley RF, et al. Darapladib, a reversible lipoprotein-associated phospholipase A2 inhibitor, for the oral treatment of atherosclerosis and coronary artery disease. IDrugs. 2009 Oct;12(10):648-55. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4998 mL | 7.4988 mL | 14.9977 mL | 37.4942 mL |
| 5 mM | 0.3000 mL | 1.4998 mL | 2.9995 mL | 7.4988 mL | |
| 10 mM | 0.1500 mL | 0.7499 mL | 1.4998 mL | 3.7494 mL | |
| 15 mM | 0.1000 mL | 0.4999 mL | 0.9998 mL | 2.4996 mL | |
| 20 mM | 0.0750 mL | 0.3749 mL | 0.7499 mL | 1.8747 mL | |
| 25 mM | 0.0600 mL | 0.3000 mL | 0.5999 mL | 1.4998 mL | |
| 30 mM | 0.0500 mL | 0.2500 mL | 0.4999 mL | 1.2498 mL | |
| 40 mM | 0.0375 mL | 0.1875 mL | 0.3749 mL | 0.9374 mL | |
| 50 mM | 0.0300 mL | 0.1500 mL | 0.3000 mL | 0.7499 mL | |
| 60 mM | 0.0250 mL | 0.1250 mL | 0.2500 mL | 0.6249 mL | |
| 80 mM | 0.0187 mL | 0.0937 mL | 0.1875 mL | 0.4687 mL | |
| 100 mM | 0.0150 mL | 0.0750 mL | 0.1500 mL | 0.3749 mL |
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