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LOX-IN-3 dihydrochloride monohydrate
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 dihydrochloride monohydrate图片
CAS NO:2414974-55-1
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
LOX-IN-3 dihydrochloride monohydrate (Compound 33) 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,癌症和血管生成研究。
生物活性

LOX-IN-3 dihydrochloride monohydrate (Compound 33) is an orally activelysyl oxidase (LOX)inhibitor. LOX-IN-3 dihydrochloride monohydrate can be used for fibrosis,cancerand angiogenesis research[1].

IC50& Target

IC50:<1 μm (human loxl2),<10 (bovine lox)[1]

体外研究
(In Vitro)

LOX-IN-3 dihydrochloride monohydrate (Compound 33) inhibits the bovine LOX and human LOXL2 activities with IC50values of<10 μm and<1 μm, respectively[1].
LOX-IN-3 dihydrochloride monohydrate exhibits sustained inhibition of LOXL1 and LOXL2[1].
LOX-IN-3 dihydrochloride monohydrate is less active against SSAO/VAP-1 and MAO-B activities[1].

体内研究
(In Vivo)

LOX-IN-3 dihydrochloride monohydrate (Compound 33) (30 mg/kg; orally; once) inhibits lysyl oxidase activity in rats[1].
LOX-IN-3 dihydrochloride monohydrate (10 mg/kg; orally; daily for 14 days) reduces kidney fibrosis in unilateral ureteric obstruction (UUO) mice model[1].
LOX-IN-3 dihydrochloride monohydrate (15 mg/kg; orally; daily for 21 days) reduces lung fibrosis in mice[1].

Animal Model:Male Wistar rats[1]
Dosage:30 mg/kg
Administration:Oral administration, single dose
Result:Completely abolished lysyl oxidase activity. Plasma concentrations of tested compound are far below the IC50after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta).
Animal Model:Unilateral ureteric obstruction (UUO) model of acute kidney fibrosis in mice[1]
Dosage:10 mg/kg
Administration:Oral gavage, daily for 14 days
Result:Increased kidney weight and thickness and reduced the area of fibrosis.
Animal Model:C57Bl/6 mice, Bleomycin-induced lung fibrosis model
Dosage:15 mg/kg
Administration:Oral gavage, daily for 21 days
Result:Significantly reduced the Ashcroft score and the lung weight.
分子量

371.26

Formula

C13H17Cl2FN2O3S

CAS 号

2414974-55-1

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.