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LOX-IN-3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
LOX-IN-3图片
CAS NO:2409963-83-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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。
Cas No.2409963-83-1
别名(2Z)-3-氟-4-(8-喹啉磺酰基)-2-丁烯-1-胺
分子式C13H13FN2O2S
分子量280.32
溶解度DMSO : 125 mg/mL (445.92 mM; Need ultrasonic)
储存条件4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.