105219-56-5 Usage
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
Different sources of media describe the Uses of 105219-56-5 differently. You can refer to the following data:
1. Platelet activating factor (PAF) antagonist.
2. Tool to evaluate the role of PAF in experimental models of human disease.
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.
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
Check Digit Verification of cas no
The CAS Registry Mumber 105219-56-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,0,5,2,1 and 9 respectively; the second part has 2 digits, 5 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 105219-56:
(8*1)+(7*0)+(6*5)+(5*2)+(4*1)+(3*9)+(2*5)+(1*6)=95
95 % 10 = 5
So 105219-56-5 is a valid CAS Registry Number.
InChI:InChI=1/C22H22ClN5O2S/c1-14-25-26-19-13-24-21(16-4-2-3-5-18(16)23)17-12-15(31-22(17)28(14)19)6-7-20(29)27-8-10-30-11-9-27/h2-5,12H,6-11,13H2,1H3
105219-56-5Relevant articles and documents
CERTAIN PAF ANTAGONIST ANTIHISTAMINE COMBINATIONS AND METHODS
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, (2008/06/13)
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Certain PAF antagonist/antihistamine combinations and methods
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, (2008/06/13)
Methods and compositions are disclosed employing combinations of antihistamines with certain diaryl tetrahydrofuran, diaryl tetrahydrothiophene, triazolobenzodiazepine or thienotriazolodiazepine PAF--antagonist compounds in the treatment of allergic reactions.
