444291

MMP-12 Inhibitor, MMP408

The MMP-12 Inhibitor, MMP408, also referenced under CAS 1258003-93-8, controls the biological activity of MMP-12. This small molecule/inhibitor is primarily used for Protease Inhibitors applications.

• Synonym(s): MMP-12 Inhibitor, MMP408, (S)-2-(8-(Methoxycarbonylamino)dibenzo[b,d]furan-3-sulfonamido)-3-methylbutanoic acid
• Empirical Formula (Hill Notation): C₁₉H₂₀N₂O₇S
• CAS Number: 1258003-93-8
• Molecular Weight: 420.44

Properties

• Quality Level: 100
• Assay: ≥94% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: off-white
• solubility: DMSO: 100 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C

Description

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.).

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

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 2
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable