Fradafiban

Product NameFradafiban
CAS148396-36-5
MFC20H21N3O4
MW367.403
EINECS
MOL File148396-36-5.mol

Chemical Properties

Density	1.38±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
pka	4.29±0.10(Predicted)

Usage And Synthesis

Uses

Fradafiban is a nonpeptide platelet glycoprotein IIb/IIIa antagonist, which binds to the human platelet GP IIb/IIIa complex with a Kd value of 148 nM.

Definition

ChEBI: A pyrrolidinone that is pyrrolidin-2-one which is substituted at positions 3 and 5 by carboxymethyl and hydroxymethyl groups, respectively, and in which the hydrogen of the resulting alcoholic hydroxy group is replaced by a 4'-carbamimidoylbiphenyl-4-yl gr up (the S,S-diastereoisomer). A figrinogen receptor antagonist.

in vivo

Fradafiban has only very limited oral activity probably due to its high polarity and thus poor absorption after oral ingestion^[1].

References

[1] Müller TH, et al. Profound and sustained inhibition of platelet aggregation by Fradafiban, a nonpeptide platelet glycoprotein IIb/IIIa antagonist, and its orally active prodrug, Lefradafiban, in men. Circulation. 1997 Aug 19;96(4):1130-8. DOI:10.1161/01.cir.96.4.1130