105219-56-5 Usage
Description
Apafant, also known as WEB-2086, is a potent and selective antagonist of the platelet-activating factor (PAF) receptor with a Ki value of 16.3 nM. It is a white solid that exhibits a range of activities, including anti-inflammatory, anti-angiogenesis, and anti-cancer properties. Apafant also demonstrates analgesic effects in animal models of neuropathic pain and is active in vivo.
Uses
Used in Pharmaceutical Industry:
Apafant is used as a PAF antagonist for its anti-inflammatory, anti-angiogenesis, and anti-cancer activities. It helps in regulating PMNL migration and edema formation, providing a robust anti-inflammatory effect when used in combination with leukotriene antagonists.
Used in Research and Development:
Apafant serves as a valuable tool to evaluate the role of PAF in experimental models of human disease, aiding in the understanding of PAF's involvement in various pathological processes and the development of targeted therapies.
Used in Pain Management:
Apafant is used as an analgesic agent in animal models of neuropathic pain, showcasing its potential application in pain management and relief.
Used in Drug Development:
Due to its active in vivo properties, Apafant can be further explored and developed into a potential therapeutic agent for various diseases, including cancer and inflammatory conditions.
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.
