化合物 LOX-IN-3 dihydrochloride monohydrate T61479

Product Introduction
Bioactivity


英文名: LOX-IN-3 dihydrochloride monohydrate

描述: 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].

体外活性: 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].

体内活性: 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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途