CTS-1027 is a small molecule inhibitor of MMPs (IC50s: 0.3 nM, 0.5 nM for MMP2, MMP13). It has > 1,000 fold selectivity over MMP1.

MMP2:0.2 nM, MMP3:9.5 nM, MMP14:15 nM, MMP8:0.9 nM, MMP13:0.5 nM, MMP12:0.7 nM

CTS-1027 improves overall animal survival following 14 days of BDL in mice [1]. CTS-1027 effectively reduces features of cholestatic liver injury, the hepatocyte apoptosis, and markers of hepatic fibrogenesis in the BDL mouse. The terminal plasma concentration of RS-130830 is 311 nM, in male animals treated for 8 weeks. RS-130830(8 weeks; male mice ) treatment causes an 89% increase in plasma triglyceride concentration. But there is no corresponding effect in female mice treated for 12 weeks. The plaque lipid content of animals receiving RS-130830 is increased by 81% at 12 weeks, and increased by 41% at 16 weeks [2].