CysLT1 Antagonist Q8 Usage And Synthesis

Description

Q8 is a novel cysteinyl leukotreine receptor antagonist, inhibiting VEGF-independent angiogenesis and exerting an additive anti-angiogenic response with bevacizumab.

Uses

Q8, an effective antiangiogenic drug, is a CysLt1 antagonist (IC50 of 4.9 μM). Q8 is sufficient to reduce cellular levels of NF-κB and calpain-2 and secreted levels of the proangiogenic proteins intercellular adhesion molecule-1, vascular cell adhesion protein-1, and VEGF[1].

References

[1] Clare T Butler, et al. A Quininib Analogue and Cysteinyl Leukotriene Receptor Antagonist Inhibits Vascular Endothelial Growth Factor (VEGF)-independent Angiogenesis and Exerts an Additive Antiangiogenic Response with Bevacizumab. J Biol Chem. 2017 Mar 3;292(9):3552-3567. DOI:10.1074/jbc.M116.747766