Antagonist of the cysteinyl leukotriene receptor 1 and 2 (CysLT1-2; IC50 values 1.4 μM and 38.5 μM, respectively). Quininib robustly inhibits developmental angiogenesis in zebrafish (at 4-10 μM), and significantly inhibits angiogenic tubule formation in HMEC-1 cells, angiogenic sprouting in aortic ring explants and retinal revascularisation in OIR mice, independently of VEGF receptors. Moreover, using ex vivo human CRC explants, Quininib significantly reduced the secretions of angiogenic growth factors and inflammatory cytokines IL-6, IL-8, VEGF, ENA-78, GRO-α, TNF, IL-1β and MCP-1.
KEYWORDS: Quininib | supplier | CysLT antagonist | 2-[(E)-2-(Quinolin-2-yl)vinyl]phenol | CAS [143816-42-6] | Cysteinyl leukotrienes | CysLT1 | CysLT2 | GPCR | VEGF | angiogenesis | LTD4 | LTE4 | blood vessels | retina | ocular | colorectal cancer | CRC