WEB 2086

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Cat.No. 2339 - WEB 2086 | C22H22N5O2SCl | CAS No. 105219-56-5
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)
Datasheet
Citations (6)
Reviews
Literature (3)

Biological Activity

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.

Compound Libraries

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Technical Data

M. Wt 455.96
Formula C22H22N5O2SCl
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 105219-56-5
PubChem ID 65889
InChI Key JGPJQFOROWSRRS-UHFFFAOYSA-N
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

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

Preparing Stock Solutions

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

Certificate of Analysis / Product Datasheet
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References

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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View all Platelet-Activating Factor (PAF) Receptor Antagonists

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:

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

Gabl et al (2014) A pepducin derived from the third intracellular loop of FPR2 is a partial agonist for direct activation of this receptor in neutrophils but a full agonist for cross-talk triggered reactivation of FPR2. PLoS One 9 e109516 PMID: 25303226

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

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


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Literature in this Area

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