PAT-1251 Hydrochloride
PAT-1251Hydrochloride是一种口服有效的选择性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1.17μM，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0.16μM。
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包装价格促销价数量
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5mg￥6950.005560.00- +
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10mg￥10162.008130.00- +
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25mg￥20662.0016530.00- +
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50mg￥31250.0025000.00- +
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100mg￥47687.0038150.00- +
- 货号: ajce48140
- CAS: 2098884-53-6
- 别名:
- 分子式: C18H18ClF4N3O3
- 分子量: 435.8
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
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.
