Apafant

ChemicalBook > CAS DataBase List > Apafant

Product Name: 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
Formula Weight: 455.96
MOL File: 105219-56-5.mol

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Apafant Property

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.

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Safety

WGK Germany: 3
Toxicity: LD50 in mice (mg/kg): 540 i.v.; 4600 orally (Casals-Stenzel)

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H361Suspected of damaging fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Sigma-Aldrich

Product number: SML0238
Product name: WEB2086
Purity: ≥98% (HPLC)
Packaging: 5mg
Price: $158
Updated: 2024/03/01

Sigma-Aldrich

Product number: SML0238
Product name: WEB2086
Purity: ≥98% (HPLC)
Packaging: 25mg
Price: $631
Updated: 2024/03/01

Cayman Chemical

Product number: 14532
Product name: Apafant
Purity: ≥98%
Packaging: 1mg
Price: $50
Updated: 2024/03/01

Cayman Chemical

Product number: 14532
Product name: Apafant
Purity: ≥98%
Packaging: 5mg
Price: $122
Updated: 2024/03/01

Tocris

Product number: 2339
Product name: WEB2086
Purity: ≥99%(HPLC)
Packaging: 1
Price: $127
Updated: 2021/12/16

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Apafant Chemical Properties,Usage,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

Raw materials

Preparation Products

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Apafant Suppliers

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View Lastest Price from Apafant manufacturers

Career Henan Chemica Co

Product: Apafant 105219-56-5
Price: US $1.00/KG
Min. Order: 1KG
Purity: MIn98%HPLC/LC
Supply Ability: 100KGS
Release date: 2020-10-29

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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

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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

WEB 2086

Apafant

1-Propanone, 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)-

105219-56-5

C22H22ClN5O2S

C22H22N5O2SCl

PAF receptor

Intermediates & Fine Chemicals

Pharmaceuticals

Sulfur & Selenium Compounds