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Description: Potent lp-PLA2 inhibitor
Chemical Name: N-[2-(Diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-4,5,6,7-tetrahydro-4-oxo-N-[[4'-(trifluoromethyl)[1,1'-biphenyl]-4-yl]methyl]-1H-cyclopentapyrimidine-1-acetamide
Purity: ≥98% (HPLC)

Biological Activity for Darapladib

Darapladib is a potent lipoprotein-associated phospholipase A2 (lp-PLA2) inhibitor (IC50 = 5 nM in whole human plasma).

Compound Libraries for Darapladib

Darapladib is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Darapladib

M. Wt 666.77
Formula C36H38F4N4O2S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 356057-34-6
PubChem ID 9939609
Smiles CCN(CCN(C(CN1C2=C(C(N=C1SCC3=CC=C(C=C3)F)=O)CCC2)=O)CC4=CC=C(C5=CC=C(C(F)(F)F)C=C5)C=C4)CC

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Darapladib

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 66.68 100
ethanol 66.68 100

Preparing Stock Solutions for Darapladib

The following data is based on the product molecular weight 666.77. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.5 mL 7.5 mL 15 mL
5 mM 0.3 mL 1.5 mL 3 mL
10 mM 0.15 mL 0.75 mL 1.5 mL
50 mM 0.03 mL 0.15 mL 0.3 mL

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Product Datasheets for Darapladib

Certificate of Analysis / Product Datasheet
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References for Darapladib

References are publications that support the biological activity of the product.

Blackie et al (2003) The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2. Bioorg.Med.Chem.Lett. 13 1067 PMID: 12643913

If you know of a relevant reference for Darapladib, please let us know.

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Keywords: Darapladib, Darapladib supplier, SB480848, lipoprotein, associated, phospholipase, A2, inhibitors, inhibits, potent, lpPLA2, lp-PLA2, Phospholipases, 6755, Tocris Bioscience

Citations for Darapladib

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