Description | PAT-1251 is an inhibitor of LOXL2 with IC50s of 10, 0.12, and 0.16 μM for the mouse, rat, and dog and can be used in studies about fibrotic diseases. |
In vitro | PAT-1251对hLOXL2及hLOXL3的抑制作用分别具有IC50值0.71 μM和1.17 μM,对LOXL2的选择性较高。与其他胺氧化酶(如SSAO、DAO、MAO-A和MAO-B)相比,PAT-1251 在10μM浓度下抑制率<10%[1]。 |
Target activity | LOXL3 (human):1.17 μM, LOXL2 (dog):0.16 μM, LOXL2 (rat):0.12 μM, LOXL2 (mouse):0.10 μM, LOXL2 (human):0.71 μM |
molecular weight | 399.34 |
Molecular formula | C18H17F4N3O3 |
CAS | 2007885-39-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
Solubility | DMSO: 117.0 mg/mL (293.0 mM) H2O: 90.0 mg/mL (225.4 mM) |
References | 1. Rowbottom MW, et al. Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2). J Med Chem. 2017 May 25;60(10):4403-4423. |