193022-04-7CTS-1027

产品属性：

Cas No.193022-04-7

别名 RS 130830;Ro 1130830;CTS1027;CTS 1027;RS130830;Ro1130830;RS-130830;Ro-1130830

化学名 4-[[4-(4-chlorophenoxy)phenyl]sulfonylmethyl]-N-hydroxyoxane-4-carboxamide

分子式 C19H20ClNO6S

分子量 425.88

溶解度 Soluble in DMSO

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
CTS-1027 is a selective inhibitor of MMP with IC50 value of 0.4 nM for MMP 2 and 0.6 nM for MMP13 [1].

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 [2] [3].

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 [4].

References:

[1].    Barta, T.E., et al., Selective, orally active MMP inhibitors with an aryl backbone. Bioorg Med Chem Lett, 2001. 11(18): p. 2481-3.

[2].    Toth, M., A. Sohail, and R. Fridman, Assessment of gelatinases (MMP-2 and MMP-9) by gelatin zymography. Methods Mol Biol, 2012. 878: p. 121-35.

[3].    Roomi, M.W., et al., Patterns of MMP-2 and MMP-9 expression in human cancer cell lines. Oncol Rep, 2009. 21(5): p. 1323-33.

[4].    Kahraman, A., et al., Matrix metalloproteinase inhibitor, CTS-1027, attenuates liver injury and fibrosis in the bile duct-ligated mouse. Hepatol Res, 2009. 39(8): p. 805-13.