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。

PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC 50 of <40 nM for LOXL2 across all mammalian species and an IC 50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride could reduce crosslinks and ameliorates fibrosis.

Solid

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 . has not independently confirmed the accuracy of these methods. They are for reference only.

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 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. has not independently confirmed the accuracy o

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[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.

In Vitro: DMSO : 125 mg/mL (284.77 mM; ultrasonic and warming and heat to 60°C)配制储备液