ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 shows anti-hepatofibrosis effects and reduces CCl4-induced hepatic fibrosis level prominently.
体外研究
ATX inhibitor 5 (compound 10g) (IC50s=1.21 and 0.78 μM) displays activities against cardiac fibroblasts (CFs) and hepatic stellate cell (HSC).
ATX inhibitor 5 at 10 μM successfully suppresses collagen content induced by TGF-β.
Cell Proliferation Assay
Cell Line:
CFs and t-HSC/Cl-6 cells
Concentration:
0.0001, 0.01, 1, 100, 10000 µM
Incubation Time:
48 hours
Result:
Displayed activities against CFs and t-HSC/Cl-6 cells with IC50s of 1.21 and 0.78 µM, respectively.
体内研究
ATX inhibitor 5 (20-40 mg/kg; p.o.; once daily for two weeks) reduces CCl4-induced hepatic fibrosis level prominently.