Merck, 444291-5MG, MMP-12 Inhibitor, MMP408

General description
A dibenzofuranylsulfanamido-valine compound that acts as a potent, active site zinc-targeting, MMP-12-selective inhibitor (IC₅₀ = 2 nM against human MMP-12) with much weaker activity against MMP-12 from mouse/rat/sheep species (IC₅₀ = 160, 320 and 22.3 nM , respectively) or human MMP-3/13/14 (IC₅₀ = 351, 120 and 1100 nM , respectively), and practically ineffective toward human Agg-1/2 (IC₅₀ >5 µM), TACE (IC₅₀ >25 µM), and MMP-1/7 (IC₅₀ >6 µM). MMP408 is orally active in mice and shown to effectively alleviate rhMMP-12-induced pulmonary inflammatory response in mice in vivo by more than 50% (5 mg/kg, p.o., b.i.d.).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Li, W., et al. 2009. J. Med. Chem.52, 1799.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)