Key result
SQ311, a novel factor Xa inhibitor utilizing a 1-aminoisoquinoline P1 ligand, demonstrated potent inhibition with a K(i) of 0.33 nM, good in vivo antithrombotic efficacy, and oral bioavailability.
Population
Preclinical models (in vitro factor Xa assays and in vivo antithrombotic models)
Design
Preclinical
Authors
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SQ311 shows promise as an oral factor Xa inhibitor in animals; leaves open translation to human trials.
Structure-based design replacing benzamidine with less basic mimics led to the discovery of SQ311, a potent, orally bioavailable factor Xa inhibitor.
Lam et al. (2003) studied Thrombosis. SQ311 (1-aminoisoquinoline P1 ligand) was evaluated on Factor Xa inhibition (K(i)). SQ311, a novel factor Xa inhibitor utilizing a 1-aminoisoquinoline P1 ligand, demonstrated potent inhibition with a K(i) of 0.33 nM, good in vivo antithrombotic efficacy, and oral bioavailability.
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