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| Apafant Basic information |
| Product Name: | Apafant | | Synonyms: | 4-[3-[4-(2-Chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-2-yl]-1-oxopropyl]-morpholine;WEB 208;WEB 2086BS;4-[3-[4-(2-Chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-α][1,4]diazepin-2-yl]-1-oxopropyl]-morpholine;3-[4-(2-Chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-2-yl]-1-(4-morpholinyl)-1-propanone;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;4-(2-Chlorophenyl)-9-methyl-2-(3-morpholino-3-oxopropyl)-6H-thieno[3,2- f] [1,2,4]triazolo[4,3-a][1,4]diazepine;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 | | CAS: | 105219-56-5 | | MF: | C22H22ClN5O2S | | MW: | 455.96 | | EINECS: | | Product Categories: | PAF receptor;Intermediates & Fine Chemicals;Pharmaceuticals;Sulfur & Selenium Compounds | | Mol File: | 105219-56-5.mol |
| Apafant Chemical Properties |
| Melting point | 186-188°C | | Boiling point | 720.2±70.0 °C(Predicted) | | density | 1.48 | | storage temp. | 2-8°C | | solubility | DMSO: soluble10mg/mL (clear solution) | | pka | 2.36±0.40(Predicted) | | form | powder | | color | white to beige | | Stability: | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 3 months. |
| WGK Germany | 3 | | Toxicity | LD50 in mice (mg/kg): 540 i.v.; 4600 orally (Casals-Stenzel) |
| Apafant Usage And Synthesis |
| 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 | Platelet activating factor (PAF) antagonist. | | Uses | 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 |
| Apafant Preparation Products And Raw materials |
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