PAT-1251 (Synonyms: PAT-1251; GB2064) |
| Catalog No.GC30112 |
PAT-1251 est un inhibiteur oral puissant et sélectif de la lysyl oxydase-like 2 (LOXL2), avec des IC50 de 0,71 et 1,17 μM pour hLOXL2 et hLOXL3 respectivement. Il inhibe également efficacement la LOXL2 chez la souris, le rat et le chien (IC50s de 0,10, 0,12 et 0,16 μM respectivement). PAT-1251 est utilisé dans la recherche sur les maladies fibrotiques.
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Cas No.: 2007885-39-2
Sample solution is provided at 25 µL, 10mM.
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PAT-1251 is a potent, selective and oral Lysyl Oxidase-Like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 has entered clinical development with the potential to treat a number of fibrotic diseases.
PAT-1251 is a Lysyl Oxidase-Like 2 (LOXL2) inhibitor, with IC50s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC50s, 0.10, 0.12, and 0.16 μM, respectively). PAT-1251 shows highly selective for LOXL2 over other key members of the amine oxidase family, such as the copper-dependent amine oxidases semicarbazide-sensitive amine oxidase (SSAO) and diamine oxidase (DAO), in addition to the flavin-dependent monoamine oxidases A (MAO-A) and B (MAO-B), with <10% inhibition at 10 μM[1].
[1]. Rowbottom MW, et al. Identification of 4-(Aminomethyl)-6-(trifluoromethyl)-2-(phenoxy)pyridine Derivatives as Potent, Selective, and Orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2). J Med Chem. 2017 May 25;60(10):4403-4423.
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