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。
货号:ajcx33768
CAS:2409963-83-1
分子式:C13H13FN2O2S
分子量：280.32
溶解度:DMSO : 125 mg/mL (445.92 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

LOX-IN-3 is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 can be used for fibrosis, cancer and/or angiogenesis research[1].

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[1].

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)[1].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[1].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[1].

[1]. Alison Dorothy Findlay, et al. Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereof. WO2020024017A1.