| Description | Lenumlostat is an orally available, selective and potent lysyl oxidase-like protein 2 (LOXL2) inhibitor with inhibitory effects on hLOXL2, hLOXL3 and LOXL2 for the study of fibrotic diseases. |
| In vitro | Lenumlostat(PAT-1251)是一种Lysyl Oxidase-Like 2 (LOXL2)抑制剂，对hLOXL2和hLOXL3的IC50分别为0.71 μM和1.17 μM。它在小鼠、大鼠和狗体内对LOXL2的抑制作用也十分强大，其IC50分别为0.10 μM、0.12 μM和0.16 μM。Lenumlostat(PAT-1251)在对LOXL2的选择性上远高于其他重要的胺氧化酶家族成员，如铜依赖性的胺氧化酶半胱氨酸敏感胺氧化酶(SSAO)和二胺氧化酶(DAO)。此外，它对黄素依赖性的单胺氧化酶A (MAO-A)和B (MAO-B)也表现出了选择性，10 μM浓度下的抑制率不足10%[1]。 |
| Target activity | LOXL2:0.10 μM (Mouse), LOXL3 (human):1.17 μM, LOXL2 (human):0.71 μM, LOXL2:0.12 μM (Rat), LOXL2:0.16 μM (Dog) |
| Synonyms | PAT-1251, GB2064 |
| molecular weight | 399.34 |
| Molecular formula | C18H17F4N3O3 |
| CAS | 2098884-52-5 |
| Storage | store under nitrogen|Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 45 mg/mL (112.69 mM), Sonication is recommended. H2O: 80 mg/mL (200.33 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. |