888490-65-1

Upstream product

• 888490-59-3 (2S,3R)-3-Hydroxymethyl-2-(4-methoxy-phenyl)-1-piperidin-1-yl-pent-4-en-1-one 
• 888490-56-0 (2S,3R)-3-Hydroxymethyl-2-(4-methoxy-phenyl)-pent-4-enoic acid 
• 110-89-4 piperidine 

Relevant academic research and scientific papers

A cassette-dosing approach for improvement of oral bioavailability of dual TACE/MMP inhibitors

The structural features contributing to the different pharmacokinetic properties of the TACE/MMP inhibitors TNF484 and TrocadeTM were analyzed using an in vivo cassette-dosing approach in rats. This enabled us to identify a new lead compound with excellent pharmacokinetic properties, but weaker activity on the biological targets. Directed structural modifications maintained oral bioavailability and restored biological activity, leading to a novel compound almost equipotent to TNF484 in vivo, but with a more than tenfold higher oral bioavailability.