PAT-1251 Hydrochloride |
Katalog-Nr.GC31949 |
PAT-1251-Hydrochlorid ist ein potenter, selektiver und oraler Lysyloxidase-Ähnlicher 2 (LOXL2)-Inhibitor mit IC50-Werten von 0,71 und 1,17 μM fÜr hLOXL2 bzw. hLOXL3 und hemmt auch stark Maus-, Ratten- und Hund-LOXL2 (IC50-Werte, 0,10 , 0,12 bzw. 0,16 μM).
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Cas No.: 2098884-53-6
Sample solution is provided at 25 µL, 10mM.
PAT-1251 Hydrochloride 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 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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