WEB 2086 (Apafant) (Synonyms: WEB 2086) |
Catalog No.GC14161
One-Click Copy Product Info
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WEB 2086 (WEB 2086), a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 105219-56-5
Sample solution is provided at 25 µL, 10mM.
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WEB 2086 (Apafant) is a water-soluble, selective, and potent platelet-activating factor (PAF) antagonist, with a Ki value of 9.9nM[1]. By targeting PAF, WEB 2086 reduces thromboxane B2, leukotriene C4, and histamine levels and prevents increases in microvascular permeability[2]. WEB 2086 has been widely used in animal models of asthma to restrain microvascular leakage and excessive mucus secretion[3].
In vitro, WEB 2086 treatment for 72 hours significantly suppressed the proliferation of MCF-7, MDA-MB-231, and HT-1080 cells, with IC50 values of 650µM, 410µM, and 380µM, respectively[4]. Incubation with 1mM WEB 2086 for 3 days induced apoptosis in NB4 cells, accompanied by extensive nuclear fragmentation, DNA fragmentation, and caspase-3 activation[5]. 1mM of WEB 2086 incubation for 5 days reduced the growth and hemoglobin accumulation of murine erythroleukemia cells (MELCs), enhanced the expression of globin genes, and downregulated the expression of c-Myb[6].
In vivo, daily intraperitoneal injection of WEB 2086 at a dose of 5mg/kg for 10 days alleviated laser-induced choroidal neovascularization (CNV) in mice, decreased the infiltration of macrophages in the retinal pigment epithelium-choroid complex[7]. One hour before antigen challenge, an oral administration of WEB 2086 (100mg/kg) markedly mitigated the airway response in guinea pigs[8].
References:[1] Kato M, Imoto K, Miyake H, et al. Apafant, a potent platelet-activating factor antagonist, blocks eosinophil activation and is effective in the chronic phase of experimental allergic conjunctivitis in guinea pigs[J]. Journal of pharmacological sciences, 2004, 95(4): 435-442.
[2] Akagi M, Nishioka E, Kanoh R, et al. Inhibitor effect of apafant on bronchopulmonary responses to platelet activating factor and to antigen in rats[J]. Arzneimittel-forschung, 1997, 47(12): 1364-1369.
[3] Tamura G, Takishima T, Mue S, et al. Effect of a potent platelet-activating factor antagonist, WEB-2086, on asthma: a multicenter, double-blind placebo-controlled study in Japan[M]//Platelet-Activating Factor and Related Lipid Mediators 2: Roles in Health and Disease. Boston, MA: Springer US, 1996: 371-380.
[4] Cellai C, Laurenzana A, Vannucchi A M, et al. Growth inhibition and differentiation of human breast cancer cells by the PAFR antagonist WEB-2086[J]. British Journal of Cancer, 2006, 94(11): 1637-1642.
[5] Laurenzana A, Cellai C, Vannucchi A M, et al. WEB-2086 and WEB-2170 trigger apoptosis in both ATRA-sensitive and-resistant promyelocytic leukemia cells and greatly enhance ATRA differentiation potential[J]. Leukemia, 2005, 19(3): 390-395.
[6] Cellai C, Laurenzana A, Vannucchi A M, et al. Specific PAF antagonist WEB‐2086 induces terminal differentiation of murine and human leukemia cells[J]. The FASEB Journal, 2002, 16(7): 733-735.
[7] Zhang H, Yang Y, Takeda A, et al. A novel platelet-activating factor receptor antagonist inhibits choroidal neovascularization and subretinal fibrosis[J]. PloS one, 2013, 8(6): e68173.
[8] Ikegami K, Hata H, Fuchigami J, et al. Apafant (a PAF receptor antagonist) suppresses the early and late airway responses in guinea pigs: a comparison with antiasthmatic drugs[J]. European journal of pharmacology, 1997, 328(1): 75-81.
| Cell experiment [1]: | |
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Cell lines |
HT-1080 cells |
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Preparation Method |
HT-1080 cells were cultured in RPMI 1640 medium, supplemented with 10% fetal bovine serum, 2mM L-glutamine, 100U/ml penicillin, and 100μg/ml streptomycin at 37°C in an incubator with 5% CO2. Cells were seeded in triplicate into 96-well plates (5×103 cells/well) and allowed to adhere overnight. Cells were incubated with WEB 2086 at various concentrations (0, 1, 10, 100, 500, and 1000µM) for 72h, and cell viability was tested. |
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Reaction Conditions |
0, 1, 10, 100, 500, and 1000µM; 72h |
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Applications |
WEB 2086 treatment decreased cell viability of HT-1080 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
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Animal models |
Female C57BL/6 mice |
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Preparation Method |
Female C57BL/6 mice (7 weeks old) were housed in SPF conditions with an automatic 12h/12h light-dark cycle at a constant temperature (21±1°C). Laser photocoagulation was applied around the optic disc using a 532-nm diode laser (200mW, 0.1-s duration, 75-µm diameter) to burn the posterior pole of the retina (4 spots/eye). Only lesions in which a subretinal bubble developed were used in subsequent experiments. 10 days after photocoagulation, the mice were anesthetized and perfused with 50mg/ml of fluorescein-labeled dextran (2×106 average molecular weight). Following enucleation and fixation in 4% paraformaldehyde, corneas and lenses were removed. Mice were treated with the WEB 2086 or phosphate-buffered saline (vehicle) 1h before photocoagulation, and treatments were continued daily until the end of the study. WEB 2086 was administered intraperitoneally to mice at 5mg/kg/day. |
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Dosage form |
5mg/kg/day; 10 days; i.p. |
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Applications |
WEB 2086 treatment alleviated laser-induced CNV via the inhibition of macrophage infiltration and the expression of proangiogenic and proinflammatory factors in mice. |
| References: [1] Cellai C, Laurenzana A, Vannucchi A M, et al. Growth inhibition and differentiation of human breast cancer cells by the PAFR antagonist WEB-2086[J]. British Journal of Cancer, 2006, 94(11): 1637-1642. [2] Zhang H, Yang Y, Takeda A, et al. A novel platelet-activating factor receptor antagonist inhibits choroidal neovascularization and subretinal fibrosis[J]. PloS one, 2013, 8(6): e68173. | |
| Cas No. | 105219-56-5 | SDF | |
| Synonyms | WEB 2086 | ||
| Chemical Name | (S)-3-(4-(2-chlorophenyl)-9-methyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-2-yl)-1-morpholinopropan-1-one | ||
| Canonical SMILES | ClC1=CC=CC=C1C2=NCC3=NN=C(C)[N@@]3[C@@]4=C2C=C(CCC(N5CCOCC5)=O)S4 | ||
| Formula | C22H22N5O2SCl | M.Wt | 455.96 |
| Solubility | DMF: 14.3 mg/ml,DMSO: 16.6 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 0.25 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1932 mL | 10.9659 mL | 21.9317 mL |
| 5 mM | 438.6 μL | 2.1932 mL | 4.3863 mL |
| 10 mM | 219.3 μL | 1.0966 mL | 2.1932 mL |
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g
μL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)