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LOX-IN-3

CAS No. : 2409963-83-1

MCE 站：LOX-IN-3

产品活性：LOX-IN-3 是一种具有口服活性的赖氨酰氧化酶 (lysyl oxidase (LOX)) 抑制剂，可用于纤维化，癌症和/或血管生成研究。

研究领域：Neuronal Signaling

作用靶点：Monoamine Oxidase

In Vitro: LOX-IN-3 (Compound 33) inhibits the bovine LOX and human LOXL2 activities with IC₅₀ values of <10 μM and <1 μM, respectively. LOX-IN-3 is less active against SSAO/VAP-1 and MAO-B activities.

In Vivo: In young male Wistar rats, a single high (30 mg/kg) dose of LOX-IN-3 (Compound 33) completely abolishes lysyl oxidase activity. While plasma concentrations of LOX-IN-3 are far below the IC50 after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta).
In a 14-day unilateral ureteric obstruction (UUO) model, LOX-IN-3 (Compound 33, 10 mg/kg daily; orally) treatment increases kidney weight and thickness and reduces the area of fibrosis as measured by Picrosirius Red.
In BALB/c mice bearing hepatic fibrosis, LOX-IN-3 (Compound 33, 20 mg/kg daily, i.p.) treatment significantly reduces liver fibrosis. At the end of week 4 a mouse breast cancer cell line (4tl) is injected orthotopically. LOX-IN-3 (Compound 33) treatment significantly reduces liver fibrosis, collagen cross-links and the metastatic load in the liver.

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