For research use only. Not for therapeutic Use.
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
| Catalog Number | R066660 |
| CAS Number | 143816-42-6 |
| Molecular Formula | C17H13NO |
| Purity | ≥95% |
| IUPAC Name | 2-[(E)-2-quinolin-2-ylethenyl]phenol |
| InChI | InChI=1S/C17H13NO/c19-17-8-4-2-6-14(17)10-12-15-11-9-13-5-1-3-7-16(13)18-15/h1-12,19H/b12-10+ |
| SMILES | C1=CC=C2C(=C1)C=CC(=N2)/C=C/C3=CC=CC=C3O |
| Reference | AL Reynolds et al. Phenotype-based Discovery of 2-[(E)-2-(Quinolin-2-yl)vinyl]phenol as a Novel Regulator of Ocular Angiogenesis. J Biol Chem. 2016 Apr 1;291(14):7242-55.
O Galvin et al. A sustained release formulation of novel quininib-hyaluronan microneedles inhibits angiogenesis and retinal vascular permeability in vivo. J Control Release. 2016 Jul 10;233:198-207.
AG Murphy et al. Preclinical validation of the small molecule drug quininib as a novel therapeutic for colorectal cancer. Sci Rep. 2016 Oct 14;6:34523. |
