LOX-IN-3 dihydrochloride

Research use only, not for human use.

LOX-IN-3 dihydrochloride is an inhibitor of lysyl oxidase (LOX). LOX-IN-3 dihydrochloride inhibited bovine LOX (IC50<10 μM) and human LOXL2 (IC50<1 μM)activities.

LOX-IN-3 dihydrochloride is an inhibitor of lysyl oxidase (LOX). LOX-IN-3 dihydrochloride inhibited bovine LOX (IC50<10 μM) and human LOXL2 (IC50<1 μM)activities.(In Vitro):LOX-IN-3 dihydrochloride can be used in fibrosis, cancer and angiogenesis studies. LOX-IN-3 dihydrochloride is less active against SSAO/VAP-1 and MAO-B activities.(In Vivo):LOX-IN-3 dihydrochloride (10 mg/kg, orally) treatment increases kidney weight and thickness and reduces the area of fibrosis In a 14-day unilateral ureteric obstruction (UUO) model. LOX-IN-3 dihydrochloride (20 mg/kg i.p.) treatment significantly reduces liver fibrosis in BALB/c mice bearing hepatic fibrosis. At the end of week 4 a mouse breast cancer cell line (4tl) is injected orthotopically. LOX-IN-3 dihydrochloride treatment significantly reduced liver fibrosis, collagen cross-links and the metastatic load in the liver. LOX-IN-3 dihydrochloride (30 mg/kg) completely abolished lysyl oxidase activity in young male Wistar rats. While plasma concentrations of LOX-IN-3 dihydrochloride were far below the IC50 after 8 hours, the half-life of recovery is between 2-3 days (ear) and 24 hours (aorta).

LOX-IN-3 dihydrochloride monohydrate (Compound 33) inhibits the bovine LOX and human LOXL2 activities with IC50 values of <10 μM and <1 μM, respectively. LOX-IN-3 dihydrochloride monohydrate exhibits sustained inhibition of LOXL1 and LOXL2.LOX-IN-3 dihydrochloride monohydrate is less active against SSAO/VAP-1 and MAO-B activities.

LOX-IN-3 dihydrochloride monohydrate (Compound 33) (30 mg/kg; orally; once) inhibits lysyl oxidase activity in rats.LOX-IN-3 dihydrochloride monohydrate (10 mg/kg; orally; daily for 14 days) reduces kidney fibrosis in unilateral ureteric obstruction (UUO) mice model.LOX-IN-3 dihydrochloride monohydrate (15 mg/kg; orally; daily for 21 days) reduces lung fibrosis in mice. Animal Model:Male Wistar rats Dosage:30 mg/kg Administration:Oral administration, single dose Result:Completely abolished lysyl oxidase activity. Plasma concentrations of tested compound are far below the IC50 after 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 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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Immunology/Inflammation

Lipoxygenase

β-Lactamase

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2409964-23-2

353.24

C13H15Cl2FN2O2S

>98% (HPLC)

In Vitro:?H2O : ≥ 100 mg/mL (283.09 mM))

NC/C=C(F)/CS(=O)(C1=C2N=CC=CC2=CC=C1)=O.[H]Cl.[H]Cl

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(-20℃)

With Ice Pack

≥ 2 years