Description
CTS-1027 is an orally bioavailable and small-molecule inhibitor ofmatrix metalloproteinases (MMPs) with IC50 values of0.4 nM, 0.6 nM and 800 nM for MMP-2, MMP-13 and MMP-1, respectively.
Product Overview
CTS-1027 is a selective inhibitor of MMP with IC50 value of 0.4 nM for MMP 2 and 0.6 nM for MMP13.MMPs (matrix metalloproteinase) are zinc-dependent endopeptidases and play an important role in degrading all kinds of extracellular matrix proteins. It is well known that MMPs involve in the cleavage of cell surface receptors, the release of apoptotic ligands, and inactivation chemokine/cytokine. And MMPs also play a pivotal role in cell proliferation, migration, differentiation, angiogenesis, apoptosis and host defense. In C57/BL6 mice model suffered bile duct ligation (BDL) for 14 days, gavage CTS-1027 reduced apoptosis of hepatocyte and bile infarcts which was a histologic indicator of liver injury at the same time activated stellate cells and reduced hepatic fibrogenesis.
Synonyms
RS 130830; Ro 1130830; CTS1027; CTS 1027; RS130830; Ro1130830; RS-130830; Ro-1130830
IC50
0.4 nM; 0.6 nM; 800 nM
Molecular Formula
C19H20ClNO6S
Chemical Name
4-[[4-(4-chlorophenoxy)phenyl]sulfonylmethyl]-N-hydroxyoxane-4-carboxamide
Solubility
Soluble in DMSO
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request