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) inhibits the bovine LOX and human LOXL2 activities with IC 50 values of <10 μM and <1 μM, respectively [1]. LOX-IN-3 dihydrochloride monohydrate exhibits sustained inhibition of LOXL1 and LOXL2 [1]. LOX-IN-3 dihydrochloride monohydrate is less active against SSAO/VAP-1 and MAO-B activities [1].

LOX-IN-3 dihydrochloride monohydrate (Compound 33) (30 mg/kg; orally; once) inhibits lysyl oxidase activity in rats [1]. LOX-IN-3 dihydrochloride monohydrate (10 mg/kg; orally; daily for 14 days) reduces kidney fibrosis in unilateral ureteric obstruction (UUO) mice model [1]. LOX-IN-3 dihydrochloride monohydrate (15 mg/kg; orally; daily for 21 days) reduces lung fibrosis in mice [1]. Animal Model: Male Wistar rats [1] Dosage: 30 mg/kg Administration: Oral administration, single dose Result: Completely abolished lysyl oxidase activity. Plasma concentrations of tested compound are far below the IC 50 after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta). Animal Model: Unilateral ureteric obstruction (UUO) model of acute kidney fibrosis in mice [1] Dosage: 10 mg/kg Administration: Oral gavage, daily for 14 days Result: Increased kidney weight and thickness and reduced the area of fibrosis. Animal Model: C57Bl/6 mice, Bleomycin-induced lung fibrosis model Dosage: 15 mg/kg Administration: Oral gavage, daily for 21 days Result: Significantly reduced the Ashcroft score and the lung weight.