TK-112690

TK-112690 is a UPP1 inhibitor. TK-112690 inhibits murine small intestinal uridine phosphorylase (UPase) with an IC₅₀ of 12.5 μM and human small intestinal UPase with an IC₅₀ of 20.0 μM in vitro. TK-112690 increases plasma uridine concentration in mice. TK-112690 can be used for the study of cancer and pulmonary fibrosis^[1][2][3]. In Vivo:TK-112690 (10-30 mg/kg, i.p., 3 h before and after methotrexate (HY-14519) on Days 2-3, 4 weeks) mitigates methotrexate (MTX) (HY-14519)-induced weight loss in LPS (HY-D1056)-treated C57BL/6 mice^[2].
TK-112690 (60 mg/kg, i.p., 3 h before and after MTX on Days 2-4, 7 days) reduces MTX-induced mucosal permeability loss in C57BL/6 female mice^[2].
TK-112690 (120 mg/kg, i.p., detected at 0.08-12 h post-dose) increases plasma uridine concentration in CD-1 female mice^[2].
TK-112690 (667-3000 mg/kg/day, continuous s.c. infusion via osmotic pumps for 24-72 h) elevates plasma uridine (UR) concentration in a linear manner in BDF-1 mice^[3].
TK-112690 (60 mg/kg, i.p., twice daily with 6-8 h interval on Days 7-20) reduces pulmonary fibrosis in C57BL/6 mice with Bleomycin (HY-108345)-induced fibrosis^[3].