PAT-1251 是一种有效的，选择性的，可口服的赖氨酰氧化酶样蛋白 2 (LOXL2) 抑制剂，对 hLOXL2 和 hLOXL3 的 IC₅₀ 值分别为 0.71 和 1.17 μM，同时对小鼠、大鼠和狗 LOXL2 的抑制作用很强，IC₅₀ 值分别为 0.10，0.12 和 0.16 μM；PAT-1251 可用于多种纤维性疾病的研究。

PAT-1251 is a potent, selective and oral lysyl oxidase-like 2 (LOXL2) inhibitor, with IC 50 s of 0.71 and 1.17 μM for hLOXL2 and hLOXL3, respectively, and also potently inhibits mouse, rat, and dog LOXL2 (IC 50 s, 0.10, 0.12, and 0.16 μM, respectively); PAT-1251 is used in the research of fibrotic diseases.

Solid

IC50: 0.10 μM (Mouse LOXL2), 0.12 μM (Rat LOXL2), 0.16 μM (Dog LOXL2), 0.71 μM (hLOXL2), 1.17 μM (hLOXL3)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[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

In Vitro: DMSO : ≥ 130 mg/mL (325.54 mM)H₂O : ≥ 100 mg/mL (250.41 mM)