| Description | 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. |
| In vivo | 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]. |
| Target activity | MMP2:0.2 nM, MMP3:9.5 nM, MMP14:15 nM, MMP8:0.9 nM, MMP13:0.5 nM, MMP12:0.7 nM |
| Synonyms | RS 130830, Ro 1130830 |
| molecular weight | 425.88 |
| Molecular formula | C19H20ClNO6S |
| CAS | 193022-04-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 100 mg/mL (234.81 mM) |
| References | 1. Kahraman A, et al. Matrix metalloproteinase inhibitor, CTS-1027, attenuates liver injury and fibrosis in the bile duct-ligated mouse. Hepatol Res. 2009 Aug;39(8):805-813. 2. Johnson JL, et al. Effect of broad-spectrum matrix metalloproteinase inhibition on atherosclerotic plaque stability. Cardiovasc Res. 2006 Aug 1;71(3):586-595. |