CTS-1027 is a potent small molecule inhibitor of MMPs (IC50=0.4 nM/0.6 nM for MMP2/MMP13), displaying > 1,000 fold selectivity over MMP1.
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HazMat fee for 500 gram (Estimated)
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The upregulation of excessive matrix metalloproteinase (MMP) has been shown to contribute to the pathogenesis of human liver diseases. CTS-1027 is a reversible MMP inhibitor that shows potent inhibitory effects on human MMP2, 3, 8, 9, 12, 13 and 14 with Ki values of ≤9 nM[3]. The IC50 values of CTS-1027 for MMP2 and MMP13 are 0.4 and 0.6 nM, respectively[4]. In mice subjected to bile duct ligation (BDL), the gavage administration of CTS-1027 (10 mg/kg body weight, once a day) resulted in a 3-fold reduction in hepatocyte apoptosis compared to vehicle-treated controls. BDL mice receiving CTS-1027 treatment also showed a 5-fold decrease in the number of caspase 3/7-positive hepatocytes in comparison to the group treated with the vehicle. The daily administration of CTS-1027 also led to 60% decrease in the mRNA expressions of both α-smooth muscle actin and collagen 1α (I) in BDL mice following daily as compared to the animals treated with vehicle.
作用机制
CTS-1027 is an MMP inhibitor that demonstrates hepato-protective and anti-fibrogenic properties during cholestatic liver injury[3].
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