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WEB-2086

BML-L137

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PAF receptor ligand

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.

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Product Details

Appearance	Beige solid.
CAS	105219-56-5
Couple Target	PAF receptor
Couple Type	Ligand
Formula	C₂₂H₂₂ClN₅O₂S
Identity	Determined by 1H-NMR.
MW	456
Purity	≥98% (HPLC)
Solubility	Soluble in DMSO or ethanol.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Handling	Store dessicated.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Lipopolysaccharide Priming Exacerbates Anaphylatoxin C5a-Induced Anaphylaxis in Mice: M. Yasuda, et al.; Biol. Pharm. Bull. 46, 432 (2023), Abstract
Platelet-activating factor and protease-activated receptor 2 cooperate to promote lung inflammation through nuclear factor-kappa B transactivation: Silva, I., Almeida, A., et al.; Authorea Preprints , (2023)
Platelet-activating factor and protease-activated receptor 2 cooperate to promote neutrophil recruitment and lung inflammation through nuclear factor-kappa B transactivation: Silva, I. S., Almeida, A. D., et al.; Sci. Rep. 13, 21637 (2023), Abstract
Mouse and human eosinophils degranulate in response to platelet-activating factor (PAF) and lysoPAF via a PAF-receptor-independent mechanism: evidence for a novel receptor: Dyer, K. D., Percopo, C. M., et al.; J. Immunol. 184, 6327 (2010), Abstract
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

Last modified: May 29, 2024

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WEB-2086

BML-L137

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