Product Introduction
Bioactivity


英文名: PXS-5153A monohydrochloride

描述: PXS-5153A monohydrochloride 是一种有效的、选择性的、具有口服活性和快速起效的赖氨酰氧化酶 2/3(LOXL2/LOXL3)的双抑制剂，对几乎所有哺乳动物物种 LOXL2的 IC50均< 40 nM，对人类 LOXL3 的 IC50为63 nM。PXS-5153A monohydrochloride 可减少交联并改善纤维化。

体外活性: PXS-5153A shows an IC 50 of <40 nM for LOXL2 across all mammalian species tested. PXS-5153A also inhibits human LOXL3 with an IC 50 value of 63 nM. PXS-5153A is >40-fold selective for LOXL2 over both LOX and LOXL1 and >700-fold selective over other related amine oxidases. PXS-5153A is a fast-acting inhibitor, with enzymatic activity almost entirely blocked within 15 minutes [1].

体内活性: As expected, rhLOXL2 induces collagen oxidation in a dose-dependent manner while PXS-5153A impedes collagen oxidation in a dose-dependent manner. Therapeutic treatment of PXS-5153A substantially reduces immature crosslink formation compared with the CCl 4 treated animals. Mature crosslink formation is also reduced by PXS-5153A treatment. All groups with therapeutic treatment of PXS-5153A show a significant reduction in DHLNL formation compared to the CCl 4 treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl 4 group. In addition, the amount of fibrillar collagen is markedly augmented by disease as seen by the 2.2-fold increase in percentage coverage area by Picrosirius red staining, which is reduced by PXS-5153A [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 250 mg/mL (569.54 mM)


关键字: PXS 5153A monohydrochloride | 2125956-82-1 free base | PXS-5153A Monohydrochloride | PXS5153A monohydrochloride | PXS-5153A | 2125956-82-1