193022-04-7
中文名稱
4-[[[4-(4-氯苯氧基)苯基]磺?；鵠甲基]四氫-N-羥基-2H-吡喃-4-甲酰胺
英文名稱
CTS-1027
CAS
193022-04-7
分子式
C19H20ClNO6S
分子量
425.88
MOL 文件
193022-04-7.mol
193022-04-7 結(jié)構(gòu)式
基本信息
中文別名
MMP抑制劑(CTS-1027)4-[[[4-(4-氯苯氧基)苯基]磺?；鵠甲基]四氫-N-羥基-2H-吡喃-4-甲酰胺
英文別名
RS130830CTS-1027
RS-130830
Ro1130830
RS 130830
Ro-1130830
Ro 1130830
RS 130830, Ro-1130830
RS 130830
RO 1130830
CTS1027
CTS 1027
RS130830
RO1130830
RS-130830
RO-1130830
4-[[[4-(4-Chlorophenoxy)phenyl]sulfonyl]methyl]tetrahydro-N-hydroxy-2H-pyran-4-carboxamide
所屬類別
生物化工：激動劑抑制劑物理化學(xué)性質(zhì)
密度1.388±0.06 g/cm3(Predicted)
儲存條件Inert atmosphere,Store in freezer, under -20°C
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)9.27±0.23(Predicted)
形態(tài)A solid
顏色White to off-white
常見問題列表
生物活性
CTS-1027 是一種有效的 MMP 抑制劑，能夠作用于 MMP2 和 MMP13，IC50 值分別為 0.3 nM 和 0.5 nM。靶點(diǎn)
IC50: 0.2 nM (MMP2), 0.5 nM (MMP13), 0.7 nM (MMP12), 0.9 nM (MMP8), 9.5 nM (MMP3), 15 nM (MMP14)
體內(nèi)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.