LOX-IN-3 dihydrochloride 是口服有效的赖氨酰氧化酶抑制剂,在纤维化,癌症和/或血管生成方面有研究价值。
产品描述
LOX-IN-3 dihydrochloride is an inhibitor of lysyl oxidase (LOX). LOX-IN-3 dihydrochloride inhibited bovine LOX (IC50<10 μM) and human LOXL2 (IC50<1 μM)activities.
体外活性
LOX-IN-3 dihydrochloride can be used in fibrosis, cancer and angiogenesis studies. LOX-IN-3 dihydrochloride is less active against SSAO/VAP-1 and MAO-B activities[1].
体内活性
LOX-IN-3 dihydrochloride (10 mg/kg, orally) treatment increases kidney weight and thickness and reduces the area of fibrosis In a 14-day unilateral ureteric obstruction (UUO) model[1]. LOX-IN-3 dihydrochloride (20 mg/kg i.p.) treatment significantly reduces liver fibrosis in BALB/c mice bearing hepatic fibrosis. At the end of week 4 a mouse breast cancer cell line (4tl) is injected orthotopically. LOX-IN-3 dihydrochloride treatment significantly reduced liver fibrosis, collagen cross-links and the metastatic load in the liver[1]. LOX-IN-3 dihydrochloride (30 mg/kg) completely abolished lysyl oxidase activity in young male Wistar rats. While plasma concentrations of LOX-IN-3 dihydrochloride were far below the IC50 after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta)[1].
Cas No.
2409964-23-2
分子式
C13H15Cl2FN2O2S
分子量
353.24
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years