CTS-1027 significantly reduces the hepatocyte apoptosis, features of cholestatic liver injury, amd markers of hepatic fibrogenesis in the BDL mouse. It improves overall animal survival following 14 days of BDL in mice. In male animals treated for 8 weeks the terminal plasma concentration of RS-130830 is 311±45 nM. Treatment of male mice with RS-130830 for 8 weeks causes an 89% increase in plasma triglyceride concentration, but there is no corresponding effect in female mice treated for 12 Plaque. The lipid content of animals receiving RS-130830 is increased by 81% at 12 weeks, and increased by 41% at 16 weeks.
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IC50: 0.2 nM (MMP2), 0.5 nM (MMP13), 0.7 nM (MMP12), 0.9 nM (MMP8), 9.5 nM (MMP3), 15 nM (MMP14)
