Darapladib

• UNSPSC 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].

• Target Antigen:

  Apoptosis; Phospholipase

• Type:

  Reference compound

• Related Pathways:

  Apoptosis;Metabolic Enzyme/Protease

• Applications:

  COVID-19-immunoregulation

• Field of Research:

  Cancer; Cardiovascular Disease

• Assay Protocol:

  https://www.medchemexpress.com/Darapladib.html

• Purity:

  99.94

• Solubility:

  DMSO : ≥ 100 mg/mL

• 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

• Molecular Weight:

  666.77

• References & Citations:

  [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.|[2]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.|[3]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. |[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.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Phase 3

• CAS Number:

  356057-34-6