Quininib

Description

Quininib is an antagonist of the cysteinyl leukotriene 1 (CysLT₁) and CysLT₂ receptors (IC₅₀s = 1.4 and 52 μM, respectively). It inhibits tubule formation in HMEC-1 cells when used at concentrations of 3.16 and 10 μM and inhibits sprout formation in isolated mouse aortic rings in an ex vivo model of angiogenesis when used at 10 μM. Quininib (3 μM) decreases angiogenesis in an oxygen-induced retinopathy mouse model of ocular angiogenesis, preventing revascularization when used at concentrations of 0.5 and 3 μM, as well as increasing neovascularization and vascular density when used at 3 μM. It reduces tumor growth and inhibits angiogenesis in an HT-29 colorectal cancer mouse xenograft model when administered at a dose of 50 mg/kg every three days.

Uses

Quininib is a novel regulator of Ocular Angiogenesis, significantly inhibiting angiogenic tubule formation in HMEC-1 cells, angiogenic sprouting in aortic ring explants and retinal revascularisation in OIR mice.

Definition

ChEBI: Quininib is a styrylquinoline that is trans-2-styrylquinoline in which the the phenyl group has been substituted at position 2 by a hydroxy group. It is an anti-angiogenic compound that exerts a dose-dependent antagonism of the cysteinyl leukotriene pathway, preferentially antagonising cysteinyl leukotriene receptor 1. The major species at pH 7.3 It has a role as an angiogenesis inhibitor. It is a styrylquinoline and a member of phenols. It is functionally related to a trans-2-styrylquinoline. It is a conjugate base of a quininib(1+).