2. Metabolic Enzyme/Protease Apoptosis
  3. Phospholipase Apoptosis
  4. Darapladib

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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CAS No. : 356057-34-6

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Based on 7 publication(s) in Google Scholar

Other Forms of Darapladib:

Darapladib Related Antibodies

Top Publications Citing Use of Products

    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.

    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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    Description

    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[1][2][3][4].

    IC50 & Target

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

    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.

    Darapladib Related Antibodies

    Apoptosis Analysis[2]

    Cell Line: C6 glioma cells and U251MG cells.
    Concentration: 5 μM
    Incubation Time: 3, 6 h
    Result: Triggered cell apoptosis in glioma cells.

    Cell Cycle Analysis[2]

    Cell Line: C6 glioma cells and U251MG cells.
    Concentration: 5 μM
    Incubation Time: 6, 12 h
    Result: Induced cell cycle arrest in glioma cells.

    Western Blot Analysis[2]

    Cell Line: C6 glioma cells and U251MG cells.
    Concentration: 5 μM
    Incubation Time: 5, 15, 30, 60 and 90 min
    Result: Induced an increase in phosphorylation of ERK1/2 proteins, but reduced AKT phosphorylation in glioma cells.
    In Vivo

    Darapladib (50 mg/kg; p.o.; once daily for 6 weeks) significantly inhibits serum Lp-PLA2 activity in LDLR-deficient mice[3].
    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.

    Animal Model: Male homozygous LDLR-deficient mice (C57/Bl6 genetic background)[3].
    Dosage: 50 mg/kg
    Administration: Oral administration; once daily for 6 weeks.
    Result: Significantly inhibited activity of serum Lp-PLA2.
    Clinical Trial
    Molecular Weight

    666.77

    Formula

    C36H38F4N4O2S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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.

    Preparing
    Stock Solutions
    Concentration Solvent 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
    View the 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.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (3.75 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    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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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.92%

    SDS (393 KB)

    COA (248 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    References

    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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    Darapladib Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Darapladib356057-34-6SB-480848SB480848SB 480848PhospholipaseApoptosisatherosclerosiscancerglioma cellapoptosisU251MG cellssubG1 cellcycle arrestInhibitorinhibitorinhibit

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