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PXS-5153A monohydrochloride

CAS No. :

MCE 站：PXS-5153A monohydrochloride

产品活性：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LOXL2的IC₅₀ 均< 40 nM，对人类LOXL3 的IC₅₀ 为63 nM。PXS-5153A monohydrochloride 可减少交联，改善纤维化。

研究领域：Neuronal Signaling

作用靶点：Monoamine Oxidase

In Vitro: PXS-5153A exhibits an IC₅₀ of <40 nM for LOXL2 across all mammalian species tested. PXS-5153A also inhibits human LOXL3 with an IC₅₀ 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 .

In Vivo: As expected, rhLOXL2 dose-dependently induce oxidation of collagen with PXS-5153A dose-dependently impeding collagen oxidation. Therapeutic treatment of PXS-5153A substantially reduces immature crosslink formation compared with the CCl₄ 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 CCl₄ treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl₄ 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.

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