Product IntroductionBioactivity英文名:
PXS-5120A描述: PXS-5120A 是一种不可逆的 Lysyl Oxidase-like 2/3 (LOXL2/3) 的氟代烯丙胺抑制剂,具有抗纤维化活性。
体外活性: PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8)[1]. 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(IC50s of 5 nM, 9 nM, 6 nM, 6 nM, 13 nM, 16 nM and 280 nM, respectively)[1].
体内活性: In mice, PXS-5129A is readily absorbed following oral gavage, and 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), while remaining well below the IC50 for LOX throughout[1].
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 50 mg/mL (103.74 mM)
关键字:
inhibit |
MAO |
Monoamine Oxidase |
Inhibitor |
PXS-5120A |
PXS5120A |
PXS 5120A相关产品:
ETAP |
J-147 |
Phenelzine sulfate |
Lysyl hydroxylase 2-IN-2 |
Safinamide mesylate |
MAO-B-IN-22 |
Paeonol |
Methyl piperate |
Rosmarinic acid |
Osthenol相关库:
Anti-Neurodegenerative Disease Compound Library |
Mitochondria-Targeted Compound Library |
Bioactive Compounds Library Max |
Antidepressant Compound Library |
Neuronal Signaling Compound Library |
Inhibitor Library |
Bioactive Compound Library