Description
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.
Product information
CAS Number: 2409964-23-2
Molecular Weight: 353.24
Formula: C13H15Cl2FN2O2S
Chemical Name: (2Z)-3-fluoro-4-(quinoline-8-sulfonyl)but-2-en-1-amine dihydrochloride
Smiles: Cl.Cl.NC/C=C(\F)/CS(=O)(=O)C1C=CC=C2C=CC=NC2=1
InChiKey: YYYHSAUHJBNINZ-LEOXJOGCSA-N
InChi: InChI=1S/C13H13FN2O2S.2ClH/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;2*1H/b11-6-;;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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/VAP-1 and MAO-B activities.
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). 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. 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.
Products are for research use only. Not for human use.
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