LOX-IN-3 dihydrochloride

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LOX-IN-3 dihydrochloride 

LOX-IN-3 dihydrochloride 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。

LOX-IN-3 dihydrochloride

LOX-IN-3 dihydrochloride Chemical Structure

CAS No. : 2409964-23-2

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LOX-IN-3 dihydrochloride 的其他形式现货产品:

LOX-IN-3

生物活性

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

体外研究
(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>[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(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)[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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

353.24

Formula

C13H15Cl2FN2O2S

CAS 号

2409964-23-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

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

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