CTS-1027
产品说明书
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同义名 : | Ro 1130830; RS 130830 |
| CAS号 : | 193022-04-7 | |
| 货号 : | A803213 | |
| 分子式 : | C19H20ClNO6S | |
| 纯度 : | 99% | |
| 分子量 : | 425.88 | |
| MDL号 : | MFCD16657131 | |
| 存储条件： |
Pure form Inert atmosphere, store in freezer, under -20°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.35mL 0.47mL 0.23mL |
11.74mL 2.35mL 1.17mL |
23.48mL 4.70mL 2.35mL |
| 参考文献 |
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