PAF receptor antagonist. Inhibits PAF-induced human platelet and neutrophil aggregation in vitro (IC50=0.17 and 0.36µM respectively). In vivo it dose dependently blocks eosinophil activation and displays antiallergic and anti-inflammatory activity in various models. Induces differentiation and triggers apoptosis and in a variety of cell lines.
Product Details
| Formula: | C22H22ClN5O2S |
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| MW: | 456 |
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| CAS: | 105219-56-5 |
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| Purity: | ≥98% (HPLC) |
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| Identity: | Determined by 1H-NMR. |
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| Appearance: | Beige solid. |
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| Solubility: | Soluble in DMSO or ethanol. |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | +4°C |
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| Handling: | Store dessicated. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
WEB-2086 and WEB-2170 trigger apoptosis in both ATRA-sensitive and -resistant promyelocytic leukemia cells and greatly enhance ATRA differentiation potential: A. Laurenzana, et al.; Leukemia
19, 390 (2005),
Abstract;
Apafant, a potent platelet-activating factor antagonist, blocks eosinophil activation and is effective in the chronic phase of experimental allergic conjunctivitis in guinea pigs: M. Kato, et al.; J. Pharmacol. Sci.
95, 435 (2004),
Abstract;
Platelet-activating factor induces lung inflammation and leak in rats: hydrogen peroxide production along neutrophil-lung endothelial cell interfaces: Y.M. Lee, et al.; J. Lab. Clin. Med.
140, 312 (2002),
Abstract;
Specific PAF antagonist WEB-2086 induces terminal differentiation of murine and human leukemia cells: C. Cellai, et al.; FASEB J.
16, 733 (2002),
Abstract;
Full Text
Pharmacological actions of WEB 2086, a new specific antagonist of platelet activating factor: J. Casals-Stenzel, et al.; J. Pharmacol. Exp. Ther.
241, 974 (1987),
Abstract;
