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].
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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. |
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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. |