PXS-5153A is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic(LOXL2/LOXL3)inhibitor, with anIC₅₀of<40 nm for loxl2 across all mammalian species and anIC₅₀of 63 nM for human LOXL3. PXS-5153A could reduce crosslinks and ameliorates fibrosis.

IC50:<40 nm (loxl2 across all mammalian species), 63 (human loxl3)^[1].

PXS-5153A exhibits an IC₅₀of<40 nm for loxl2 across all mammalian species tested. pxs-5153a also inhibits human loxl3 with an ic₅₀value 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].

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 CCl₄treated 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 CCl₄treated animals. Treatment with PXS-5153A causes a significantly reduction in HYP compared to the CCl₄group. 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].

475.41

C₂₀H₂₅Cl₂FN₄O₂S

2125956-82-1

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