| 产品描述: | LOX-IN-3 is an orally active lysyl oxidase (LOX) inhibitor. LOX-IN-3 can be used for fibrosis, cancer and angiogenesis research |
| 靶点: |
IC50: <1 μM (human LOXL2), <10 μM (bovine LOX) |
| 体外研究: |
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. |
| 体内研究: |
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[1]Dosage: 10 mg/kgAdministration: Oral gavage, daily for 14 daysResult: Increased kidney weight and thickness and reduced the area of fibrosis.Animal Model: C57Bl/6 mice, Bleomycin-induced lung fibrosis modelDosage: 15 mg/kgAdministration: Oral gavage, daily for 21 daysResult: Significantly reduced the Ashcroft score and the lung weight. |
| 参考文献: |
1. Alison Dorothy Findlay, et al. Haloallylamine sulfone derivative inhibitors of lysyl oxidases and uses thereof. WO2020024017A1. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
3.567 ml |
17.837 ml |
35.674 ml |
| 5 mM |
0.713 ml |
3.567 ml |
7.135 ml |
| 10 mM |
0.357 ml |
1.784 ml |
3.567 ml |
| 50 mM |
0.071 ml |
0.357 ml |
0.713 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |