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

Product Specifications

CAS Number

[356057-34-6]

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.