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Submit ReviewWEB 2086
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)
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 |
| 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 for WEB 2086
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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:
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
Yagnik (2014) Macrophage derived platelet activating factor implicated in the resolution phase of gouty inflammation. Int J Inflam 2014 526496 PMID: 25328755
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
Do you know of a great paper that uses WEB 2086 from Tocris? Please let us know.
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