Apafant
- CAS No.
- 105219-56-5
- Chemical Name:
- Apafant
- Synonyms
- WEB 208;Apafant;WEB 2086;WEB 2086BS;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-[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-α][1,4]diazepin-2-yl]-1-oxopropyl]-morpholine;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;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
- CBNumber:
- CB5252385
- Molecular Formula:
- C22H22ClN5O2S
- Molecular Weight:
- 455.96
- MDL Number:
- MFCD00865271
- MOL File:
- 105219-56-5.mol
- MSDS File:
- SDS
| 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. |
| FDA UNII | J613NI05SV |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS08 |
|---|---|
| Signal word | Warning |
| Hazard statements | H361 |
| Precautionary statements | P201-P202-P281-P308+P313-P405-P501 |
| WGK Germany | 3 |
| Toxicity | LD50 in mice (mg/kg): 540 i.v.; 4600 orally (Casals-Stenzel) |
Apafant price More Price(15)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML0238 | WEB2086 ≥98% (HPLC) | 105219-56-5 | 5mg | $158 | 2024-03-01 | Buy |
| Sigma-Aldrich | SML0238 | WEB2086 ≥98% (HPLC) | 105219-56-5 | 25mg | $631 | 2024-03-01 | Buy |
| Cayman Chemical | 14532 | Apafant ≥98% | 105219-56-5 | 1mg | $50 | 2024-03-01 | Buy |
| Cayman Chemical | 14532 | Apafant ≥98% | 105219-56-5 | 5mg | $122 | 2024-03-01 | Buy |
| Tocris | 2339 | WEB2086 ≥99%(HPLC) | 105219-56-5 | 1 | $127 | 2021-12-16 | Buy |
Apafant Chemical Properties,Uses,Production
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.
Definition
ChEBI: LSM-2613 is an organonitrogen heterocyclic compound and an organosulfur heterocyclic compound.
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.
storage
Desiccate at +4°C
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
Apafant Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| Hefei Hirisun Pharmatech Co., Ltd | +8615056975894 | shawn@hirisunpharm.com | CHINA | 9923 | 58 |
| Alfa Chemistry | +1-5166625404 | Info@alfa-chemistry.com | United States | 21317 | 58 |
| Hebei Duling International Trade Co. LTD | +8618032673083 | sales05@hbduling.cn | China | 15745 | 58 |
| Hangzhou MolCore BioPharmatech Co.,Ltd. | +86-057181025280; +8617767106207 | sales@molcore.com | China | 49739 | 58 |
| Nantong HI-FUTURE Biology Co., Ltd. | +undefined18051384581 | sales@chemhifuture.com | China | 3136 | 58 |
| SUZHOU SENFEIDA CHEMICAL CO.,LTD | +86-0512-83500002 +8615195660023 | sales@senfeida.com | China | 5100 | 58 |
| Aladdin Scientific | +1-833-552-7181 | sales@aladdinsci.com | United States | 52927 | 58 |
