Darapladib

• 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].

• Product Name Alternative :

  SB-480848

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  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 :

  99.92

• 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 Formula :

  C36H38F4N4O2S

• Molecular Weight :

  666.77

• Precautions :

  H302, H315, H319, H335

• 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)

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 3

• CAS Number :

  [356057-34-6]