| Description | PXS-5153A is an effective, selective, and fast-acting inhibitor of lysyl oxidase like 2/3 enzymes with enzymatic activity almost entirely blocked within 15 minutes. PXS-5153A could reduce crosslinks and ameliorates fibrosis. |
| In vitro | PXS-5153A对LOXL2的选择性是针对LOX和LOXL1的>40倍，以及对其他相关胺氧化酶的>700倍。 对于所有已测试的哺乳动物物种，PXS-5153A对LOXL2的IC50值<40 nM。PXS-5153A还能抑制人类LOXL3，其IC50值为63 nM[1]。 |
| In vivo | rhLOXL2能剂量依赖性促进胶原蛋白氧化，而PXS-5153A同样剂量依赖性抑制胶原蛋白氧化。与CCl4处理的动物相比，PXS-5153A的治疗显著减少未成熟交联的形成。PXS-5153A治疗也减少了成熟交联的形成。所有接受PXS-5153A治疗的组在DHLNL形成和HYP上，与CCl4处理的动物相比都有显著减少[1]。 |
| Target activity | LOXL3:63 nM (human), LOXL2:<40 nM (across all mammalian species) |
| molecular weight | 475.41 |
| Molecular formula | C20H25Cl2FN4O2S |
| CAS | 2125956-82-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 20 mg/mL DMSO: 45 mg/mL (94.66 mM) |
| References | 1. Schilter H, et al. The lysyl oxidase like 2/3 enzymatic inhibitor, PXS-5153A, reduces crosslinks and ameliorates fibrosis. J Cell Mol Med. 2018 Dec 9. |