| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 100 mg/mL (283.09 mM; Need ultrasonic) | [form ]
Solid | [color ]
Off-white to light yellow | [InChI]
InChI=1S/C13H13FN2O2S.ClH/c14-11(6-7-15)9-19(17,18)12-5-1-3-10-4-2-8-16-13(10)12;/h1-6,8H,7,9,15H2;1H/b11-6-; | [InChIKey]
WEFLTRNHDTUNKA-AVHZNCSWSA-N | [SMILES]
S(C1=CC=CC2C=CC=NC1=2)(=O)(=O)C/C(/F)=C/CN.Cl |
| Hazard Information | Back Directory | [Uses]
LOX-IN-3 dihydrochloride is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 dihydrochloride can be used for fibrosis, cancer and angiogenesis research[1]. | [Biological Activity]
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].
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]. | [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 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[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. |
| [storage]
Store at -20°C | [References]
[1]. Alison Dorothy Findlay, et al. Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereof. WO2020024017A1. |
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| Company Name: |
InvivoChem
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| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
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