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 (4)
Literature

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 45.6 100
ethanol 45.6 100mM 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 solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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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Safety Datasheet

References

References are publications that support the products' biological activity.

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, supplier, Potent, PAF, receptor, antagonists, Receptors, Platelet-activating, Factor, WEB2086, Apafant, Platelet-activating, Factor, (PAF), Receptors, Platelet-activating, Factor, (PAF), Receptors, Tocris Bioscience

4 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

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

Yagnik (2014) Macrophage derived platelet activating factor implicated in the resolution phase of gouty inflammation. Int J Inflam 2014 526496 PMID: 25328755

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


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