LOX-IN-3 (C09-1142-554)

LOX-IN-3 is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 can be used for fibrosis, cancer and angiogenesis researchIn VitroLOX-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. LOX-IN-3 dihydrochloride monohydrate exhibits sustained inhibition of LOXL1 and LOXL2. LOX-IN-3 dihydrochloride monohydrate is less active against SSAO/VAP-1 and MAO-B activities. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoLOX-IN-3 dihydrochloride monohydrate (Compound 33) (30 mg/kg; orally; once) inhibits lysyl oxidase activity in rats . LOX-IN-3 dihydrochloride monohydrate (10 mg/kg; orally; daily for 14 days) reduces kidney fibrosis in unilateral ureteric obstruction (UUO) mice model . LOX-IN-3 dihydrochloride monohydrate (15 mg/kg; orally; daily for 21 days) reduces lung fibrosis in mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Wistar rats 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 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.Form:SolidIC50& Target:IC 50 : <1 μM (human LOXL2), <10 μM (bovine LOX). Molecular Formula: C13H13FN2O2S Molecular Weight: 280.32 PubChem CID: 146317833 Isomeric SMILES: C1=CC2=C(C(=C1)S(=O)(=O)C/C(=C/CN)/F)N=CC=C2