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WEB-2086 | PAF receptor antagonist

CAS:
105219-56-5
Catalog Number:
10-1389
Activity:
PAF receptor antagonist
Alternate Names:
Apafant
Chemical Name:
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
Molecular Weight:
455.96
Molecular Formula:
C22H22ClN5O2S
Solubility:
Soluble in DMSO (greater than 50 mg/ml) or in Ethanol (up to 25 mg/ml with warming).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
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.
Shipping Code:
RT

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.

References/Citations:

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

WEB-2086 | PAF receptor antagonist is also available in the Cellular Metabolism Library.
CAS:
105219-56-5
Catalog Number:
10-1389
Activity:
PAF receptor antagonist
Alternate Names:
Apafant
Chemical Name:
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
Molecular Weight:
455.96
Molecular Formula:
C22H22ClN5O2S
Solubility:
Soluble in DMSO (greater than 50 mg/ml) or in Ethanol (up to 25 mg/ml with warming).
Physical Properties:
White solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°
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.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

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