BI 4394 is a highly potent and selective MMP-13 inhibitor (IC50 = 1 nM). BI 4394 inhibits the degradation of isolated bovine nasal cartilage explants (IC50 = 31 nM). It shows high selectivity (>1000 fold) for MMP-13 over other MMPs. In vivo, BI 4394 decreases the mean arthritic score vs control in a murine model of rheumatoid arthritis, when administered at a dose of 100 mg/kg over a 14-day period. BI 4394 is orally bioavailable.
- Nom chimique ou matériau
- 2-Ethyl 5-[3-[[[(4-carboxyphenyl)methyl]amino]carbonyl]-1-methyl-1H-pyrazol-5-yl]-1H-indole-2-carboxylate
- CAS
- 1222173-37-6
- Cible
- Synthetic Metalloprotease Inhibitors
- Formule moléculaire
- C24H22N4O5
- Pureté
- 0.98
