Description
WEB-2086 (105219-56-5) is a potent and selective antagonist of the platelet activating factor (PAF) receptor (Ki = 16.3 nM).1Displays an activity profile which includes antiinflammatory, antiangiogenesis and anticancer activity.2Along with leukotriene antagonists, WEB-2086 cooperatively provides a robust antiinflammatory effect regulating PMNL migration and edema formation.3Displays analgesic effects in animal models of neuropathic pain.4Active in vivo.
Chemical Properties
White Solid
Uses
Platelet activating factor (PAF) antagonist.
Uses
Tool to evaluate the role of PAF in experimental models of human disease.
Definition
ChEBI: LSM-2613 is an organonitrogen heterocyclic compound and an organosulfur heterocyclic compound.
Biological Activity
Potent, selective platelet-activating factor (PAF) receptor antagonist (K i = 16.3 nM). Displays anti-inflammatory, antiangiogenic and anticancer activity. Inhibits growth and proliferation of MCF-7 breast cancer cells.
Biochem/physiol Actions
WEB2086 is a very potent, selective platelet-activating factor (PAF) antagonist (IC50 = 16 nM). WEB2086 inhibits the proliferation of tumor cells and slows tumor growth in xenograft tumor models, and has been shown to inhibit angiogenesis.
storage
Desiccate at +4°C
References
[1] GORDON DENT . Characterization of PAF receptors on human neutrophils using the specific antagonist, WEB 2086 Correlation between receptor binding and function[J]. FEBS Letters, 1989, 244 2: Pages 365-368. DOI:
10.1016/0014-5793(89)80564-2[2] C CELLAI. Growth inhibition and differentiation of human breast cancer cells by the PAFR antagonist WEB-2086[J]. British Journal of Cancer, 2006, 94 11: 1637-1642. DOI:
10.1038/sj.bjc.6603156[3] CLAUDIA S. BITENCOURT. Cooperative role of endogenous leucotrienes and platelet-activating factor in ischaemia–reperfusion-mediated tissue injury[J]. JOURNAL OF CELLULAR AND MOLECULAR MEDICINE, 2013, 17 12: 1554-1565. DOI:
10.1111/jcmm.12118[4] N. MOTOYAMA. Pain-releasing action of Platelet-activating factor (PAF) antagonists in neuropathic pain animal models and the mechanisms of action[J]. European Journal of Pain, 2013, 17 8: 1156-1167. DOI:
10.1002/j.1532-2149.2013.00289.x
