您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > PAT-1251
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
PAT-1251
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PAT-1251图片
CAS NO:2007885-39-2
规格:98%
分子量:399.34
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
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1.17μM,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;PAT-1251已经进入临床开发,有治疗多种纤维性疾病的潜力。
CAS:2007885-39-2
分子式:C18H17F4N3O3
分子量:399.34
纯度:98%
存储:Store at -20°C

Background:

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.