Apafant Chemical Properties

Melting point:

186-188°C

Boiling point:

720.2±70.0 °C(Predicted)

Density 

1.48

storage temp. 

2-8°C

solubility 

DMSO: soluble10mg/mL (clear solution)

pka

2.36±0.40(Predicted)

form 

powder

color 

white to beige

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months.

Safety Information

WGK Germany 

3

Toxicity

LD50 in mice (mg/kg): 540 i.v.; 4600 orally (Casals-Stenzel)

Apafant Usage And Synthesis

Description

WEB-2086 (105219-56-5) is a potent and selective antagonist of the platelet activating factor (PAF) receptor (Ki = 16.3 nM).1?Displays an activity profile which includes antiinflammatory, antiangiogenesis and anticancer activity.2?Along with leukotriene antagonists, WEB-2086 cooperatively provides a robust antiinflammatory effect regulating PMNL migration and edema formation.3?Displays analgesic effects in animal models of neuropathic pain.4?Active 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) Dent et al. (1989), Characterization of PAF receptors on human neutrophils using the specific antagonist WEB 2086. Correlation between receptor binding and function; FEBS Lett., 244 365 2) Cellai et al. (2006), Growth inhibition and differentiation of human breast cancer cells by PAFR antagonist WEB-2086; Br. J. Cancer, 94 1637 3) Bitencourt et al. (2013), Cooperative role of endogenous leucotrienes and platelet-activating factor in ischaemia-reperfusion-mediated tissue injury; J. Cell. Mol. Med., 17 1554 4) Motoyama et al. (2013), Pain-releasing action of platelet-activating factor (PAF) antagonists in neuropathic pain animal models and the mechanisms of action; Eur. J. Pain, 17 1156

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