中文名称:
4-[[[4-(4-氯苯氧基)苯基]磺酰基]甲基]四氢-N-羟基-2H-吡喃-4-甲酰胺
中文同义词:
4-[[[4-(4-氯苯氧基)苯基]磺酰基]甲基]四氢-N-羟基-2H-吡喃-4-甲酰胺;MMP抑制剂(CTS-1027)
英文同义词:
CTS-1027;2H-Pyran-4-carboxaMide, 4-[[[4-(4-chlorophenoxy)phenyl]sulfonyl]Methyl]tetrahydro-N-hydroxy-;Ro 1130830;Ro1130830;Ro-1130830;RS 130830;RS130830;RS-130830
密度
1.388±0.06 g/cm3(Predicted)
储存条件
Inert atmosphere,Store in freezer, under -20°C
酸度系数(pKa)
9.27±0.23(Predicted)
生物活性
CTS-1027 是一种有效的 MMP 抑制剂，能够作用于 MMP2 和 MMP13，IC50 值分别为 0.3 nM 和 0.5 nM。
靶点
IC50: 0.2 nM (MMP2), 0.5 nM (MMP13), 0.7 nM (MMP12), 0.9 nM (MMP8), 9.5 nM (MMP3), 15 nM (MMP14)
体内研究
CTS-1027 significantly reduces the hepatocyte apoptosis, features of cholestatic liver injury, amd markers of hepatic fibrogenesis in the BDL mouse. CTS-1027 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 weeks. The plaque lipid content of animals receiving RS-130830 is increased by 81% at 12 weeks, and increased by 41% at 16 weeks.
