| Identification | Back Directory | [Name]
2-Buten-1-amine, 3-fluoro-4-(8-quinolinylsulfonyl)-, (2Z)- | [CAS]
2409963-83-1 | [Synonyms]
PXS5505
DWN63831
LOX-IN-3
LOXIN3,LOX IN 3
Lysyl oxidase inhbitor 1
2-Buten-1-amine, 3-fluoro-4-(8-quinolinylsulfonyl)-, (2Z)- | [Molecular Formula]
C13H13FN2O2S | [MDL Number]
MFCD34167539 | [MOL File]
2409963-83-1.mol | [Molecular Weight]
280.32 |
| Chemical Properties | Back Directory | [Boiling point ]
529.1±50.0 °C(Predicted) | [density ]
1.330±0.06 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO : 125 mg/mL (445.92 mM; Need ultrasonic) | [form ]
Solid | [pka]
6.96±0.29(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
LOX-IN-3 is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 can be used for fibrosis, cancer and angiogenesis research[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. |
| [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
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|