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

Darapladib  (Synonyms: SB-480848)

Cat. No.: HY-10521 Purity: 99.94%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Darapladib Chemical Structure

Darapladib Chemical Structure

CAS No. : 356057-34-6

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Solid + Solvent
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 191 In-stock
Solid
5 mg USD 130 In-stock
10 mg USD 210 In-stock
25 mg USD 420 In-stock
50 mg USD 680 In-stock
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Based on 4 publication(s) in Google Scholar

Darapladib Related Antibodies

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Phospholipase A PLD

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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

Appearance

Solid

Formula

C36H38F4N4O2S
CAS No.
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)

*"≥" 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
10 mM 0.1500 mL 0.7499 mL 1.4998 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

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

  • 3.

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

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

*All of the co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.94%

COA (248 KB) HNMR (283 KB) LCMS (265 KB)

Handling Instructions (2659 KB)
References
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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.

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Keywords:

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

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