PXS-5120A

PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 ( K i of 83 nM; pIC 50 of 8.4) over LOXL ( pIC 50 of 5.8) In Vitro PXS-5120A (Compound 12k) is a potent inhibitor of the LOXL2/3 enzyme and a moderate blocker of LOXL4. PXS-5120A inhibits recombinant human LOXL2, human fibroblast LOXL2, recombinant mouse LOXL2, recombinant rat LOXL2, collagen oxidation assay, recombinant human LOXL3 and recombinant human LOXL4 with IC 50 s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo PXS-5129A is readily absorbed following oral gavage, and once in the circulation, rapidly hydrolyzed to release PXS-5120 (free base) in vivo, affording plasma concentrations well above the LOXL2 IC 50 (6 nM) for a prolonged period (>6 h) in mice, while remaining well below the IC50 for LOX throughout . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:pKi: 8.4 (Lysyl Oxidase-like 2) and 5.8 (Lysyl Oxidase-like),Ki: 83 nM (Lysyl Oxidase-like 2)

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