Benzylacyclouridine

Benzylacyclouridine (BAU) is a potent and specific inhibitor of uridine phosphorylase, the first enzyme in the catabolism of uridine. Benzylacyclouridine inhibits the metabolic activity of UPP1 and the activity of UPP2. Benzylacyclouridine can modulate the cytotoxic side effects of 5-fluorouracil (5-FU) and its derivatives^{[1][2][3][4][5]}. IC50 & Target:uridine phosphorylase^[1] In Vitro:Benzylacyclouridine increases 5-FU-induced cytotoxicity in a number of human cancer cell lines^[1].
Benzylacyclouridine (20-100 μM) reduces the rapid clearance of trace amounts of either [¹⁴C]uridine or hyperphysiologic concentrations of non-labeled uridine by the isolated rat liver perfused with an artificial oxygen carrier^[2]. In Vivo:Benzylacyclouridine (p.o. or i.v.) arrests the rapid degradation of a tracer dose of uridine into uracil in dogs and pigs^[1].
Benzylacyclouridine exhibits the t_1/2 of 1.8-3.6 h in dogs, with bioavailability levels of 85% (30 mg/kg) and 42.5% (120 mg/kg)^[1].
Benzylacyclouridine (120 mg/kg) exhibits the t_1/2 of 1.6-2.3 h, with a bioavailability of 40% in pigs^[1].