Apafant

Apafant (WEB 2086), a chemical probe, is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Ki of 9.9 nM. Apafant increases the gene expression of PAF-r, α-globin, β-globin, decreases the c-myb gene expression. Apafant shows a protective effect on alkyl-PAF-mediated lethalit[1][2][3].

Product Specifications

CAS Number

[105219-56-5]

Product Name Alternative

WEB 2086

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Platelet-activating Factor Receptor (PAFR)

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/apafant.html

Purity

99.96

Solubility

DMSO : 40 mg/mL (ultrasonic; warming)

Smiles

O=C(N1CCOCC1)CCC(S2)=CC3=C2N4C(CN=C3C5=CC=CC=C5Cl)=NN=C4C

Molecular Formula

C22H22ClN5O2S

Molecular Weight

455.96

Precautions

H302, H315, H319, H335

References & Citations

[1]Kato M, 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 Pharmacol Sci. 2004 Aug;95 (4) :435-42.|[2]Cellai C, Laurenzana A, Vannucchi AM, Della Malva N, Bianchi L, Paoletti F. Specific PAF antagonist WEB-2086 induces terminal differentiation of murine and human leukemia cells. FASEB J. 2002 May;16 (7) :733-5.|[3]Chaithra VH, et al. Modulation of inflammatory platelet-activating factor (PAF) receptor by the acyl analogue of PAF. J Lipid Res. 2018 Nov;59 (11) :2063-2074.