Apafant-d8

Apafant-d8 is the deuterium labeled Apafant. Apafant (WEB 2086) is a potent platelet-activating factor (PAF) antagonist, inhibits PAF binding to human PAF receptors with a Kiof 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

[1185101-22-7]

UNSPSC

12352005

Target

Isotope-Labeled Compounds; Platelet-activating Factor Receptor (PAFR)

Related Pathways

GPCR/G Protein; Others

Field of Research

Inflammation/Immunology

Solubility

10 mM in DMSO

Smiles

O=C(N1C([2H])([2H])C([2H])([2H])OC([2H])([2H])C1([2H])[2H])CCC2=CC3=C(S2)N4C(CN=C3C5=C(C=CC=C5)Cl)=NN=C4C

Molecular Formula

C22H14D8ClN5O2S

Molecular Weight

464.01

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[3]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.|[4]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.