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CAS No. : 2125955-70-4
MCE 国际站:PXS-5120A
产品活性:PXS-5120A 是一种有效的,不可逆的 Lysyl Oxidase-like 2/3 (LOXL2/3) 的氟代烯丙胺抑制剂,具有抗纤维化活性。与 LOXL (pIC50 为 5.8) 相比,PXS-5120A 对 LOXL2 (Ki 为 83 nM; pIC50 为 8.4) 的选择性高 300 倍以上。
研究领域:Neuronal Signaling
作用靶点:Monoamine Oxidase
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 IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively.
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 IC50 (6 nM) for a prolonged period (>6 h) in mice, while remaining well below the IC50 for LOX throughout.
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