LOX-IN-3 dihydrochloride monohydrate (Compound 33) is an orally active lysyl oxidase (LOX) inhibitor, intended for research in fibrosis, cancer, and angiogenesis [1].

LOX-IN-3 dihydrochloride monohydrate (Compound 33) effectively inhibits bovine LOX and human LOXL2 with IC50 values of <10 μM and <1 μM, respectively, while maintaining prolonged inhibition of LOXL1 and LOXL2 and showing reduced activity against SSAO/VAP-1 and MAO-B [1].

LOX-IN-3 dihydrochloride monohydrate (Compound 33) administered at various doses and durations has shown effects on fibrosis and enzyme activity in animal models. A 30 mg/kg oral dose abolished lysyl oxidase activity in male Wistar rats, with plasma concentrations dropping below IC 50 after 8 hours and a recovery half-life of 2-3 days (ear) to 24 hours (aorta) [1]. Daily oral administration of 10 mg/kg for 14 days in a UUO model increased kidney weight and thickness while reducing fibrosis area in mice [1]. A daily oral dose of 15 mg/kg for 21 days significantly decreased lung fibrosis in C57Bl/6 mice, evidenced by reductions in the Ashcroft score and lung weight [1].