WEB 2086

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Description: Potent PAF receptor antagonist
Alternative Names: Apafant
Chemical Name: 4-[3-[4[(2-Chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a]diazepin-2-yl]-1-oxopropyl]morpholine
Purity: ≥99% (HPLC)
Citations (6)

Biological Activity for WEB 2086

WEB 2086 is a potent, selective platelet-activating factor (PAF) receptor antagonist (Ki = 16.3 nM). Displays anti-inflammatory, antiangiogenic and anticancer activity. Inhibits growth and proliferation of MCF-7 breast cancer cells.

Technical Data for WEB 2086

M. Wt 455.96
Formula C22H22N5O2SCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 105219-56-5
PubChem ID 65889
Smiles CC1=NN=C2CN=C(C3=C(SC(CCC(=O)N4CCOCC4)=C3)N12)C1=CC=CC=C1Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for WEB 2086

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 45.6 100
ethanol 45.6 100 with gentle warming

Preparing Stock Solutions for WEB 2086

The following data is based on the product molecular weight 455.96. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.19 mL 10.97 mL 21.93 mL
5 mM 0.44 mL 2.19 mL 4.39 mL
10 mM 0.22 mL 1.1 mL 2.19 mL
50 mM 0.04 mL 0.22 mL 0.44 mL

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Product Datasheets for WEB 2086

Certificate of Analysis / Product Datasheet
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References for WEB 2086

References are publications that support the biological activity of the product.

Dent et al (1989) Characterization of PAF receptors on human neutrophils using the specific antagonist, WEB 2086. FEBS Lett. 244 365 PMID: 2537761

Sariahmetoglu et al (1998) Effects of WEB 2086 on the protective role of preconditioning against arrhythmias in rats. Pharmacol.Res. 38 173 PMID: 9782066

Cellai et al (2006) Growth inhibition and differentiation of human breast cancer cells by the PAFR antagonist WEB-2086. Br.J.Cancer 94 1637 PMID: 16721373

If you know of a relevant reference for WEB 2086, please let us know.

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Keywords: WEB 2086, WEB 2086 supplier, Potent, PAF, receptor, antagonists, Receptors, Platelet-activating, Factor, WEB2086, Apafant, (PAF), 2339, Tocris Bioscience

6 Citations for WEB 2086

Citations are publications that use Tocris products. Selected citations for WEB 2086 include:

Zhao et al (2013) Important role of platelets in modulating endotoxin-induced lung inflammation in CFTR-deficient mice. Br J Pharmacol 8 e82683 PMID: 24367540

Al-Shawaf et al (2010) Short-term stimulation of calcium-permeable transient receptor potential canonical 5-containing channels by oxidized phospholipids. Arterioscler Thromb Vasc Biol 30 1453 PMID: 20378846

Ajiro et al (2011) Platelet-activating factor stimulates sodium-hydrogen exchange in ventricular myocytes. PLoS One 301 H2395 PMID: 21949111

Wu et al (2014) Lipoxin A4 and platelet activating factor are involved in E. coli or LPS-induced lung inflammation in CFTR-deficient mice. PLoS One 9 e93003 PMID: 24671173

Do you know of a great paper that uses WEB 2086 from Tocris? Please let us know.

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