LOX-IN-3 dihydrochloride monohydrate (Compound 33) is a lysyl oxidase (LOX) inhibitor with oral activity. It is specifically designed for research purposes in the areas of fibrosis, cancer, and angiogenesis [1].

LOX-IN-3 dihydrochloride monohydrate (Compound 33) effectively inhibits bovine LOX and human LOXL2, demonstrating IC 50 values of <10 μM and <1 μM, respectively [1]. This compound maintains prolonged inhibition of LOXL1 and LOXL2, while exhibiting reduced activity against SSAO/VAP-1 and MAO-B [1].

LOX-IN-3 dihydrochloride monohydrate (Compound 33), administered at different dosages and durations, has been shown to influence fibrosis and enzyme activity in various animal models. At a dosage of 30 mg/kg administered orally once, it completely abolished lysyl oxidase activity in male Wistar rats, with plasma concentrations of the compound dropping below the IC 50 after 8 hours, and recovery half-life ranging from 2-3 days (ear) to 24 hours (aorta) [1]. When given orally daily at 10 mg/kg for 14 days to mice in a unilateral ureteric obstruction (UUO) model, it resulted in increased kidney weight and thickness while reducing fibrosis area [1]. Moreover, a daily oral dose of 15 mg/kg for 21 days significantly decreased lung fibrosis in C57Bl/6 mice, as shown by reductions in both the Ashcroft score and lung weight [1].