ATX inhibitor 5

ATX inhibitor 5 is a potent and orally active autotaxin (ATX) inhibitor, with an IC50 of 15.3 nM. ATX inhibitor 5 has anti-hepatofibrosis effect, and reduces CCl4-induced hepatic fibrosis level prominently[1].

Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE)

Research Areas >> Inflammation/Immunology

Autotaxin

ATX inhibitor 5 displays anti-proliferative activities with IC50s of 1.21 and 0.78 µM, respectively[1]. Cell Proliferation Assay[1] 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.

ATX inhibitor 5 (20-40 mg/kg; p.o.; once daily for two weeks) reduces CCl4-induced hepatic fibrosis level prominently[1]. Animal Model: Male Konmin mice (8-week old, 22-25 g)[1] Dosage: 20, 40 mg/kg Administration: Orally; once daily for two weeks Result: Prominently reduced CCl4-induced hepatic fibrosis level.

[1]. Jiang N, et al.Optimization and evaluation of novel tetrahydropyrido[4,3-d]pyrimidine derivatives as ATX inhibitors for cardiac and hepatic fibrosis.Eur J Med Chem. 2020 Feb 1;187:111904.