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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
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
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 No.2007885-39-2
Canonical SMILESFC(F)(F)C1=NC(OC2=CC(C(N3C[C@@H](F)[C@H](O)C3)=O)=CC=C2)=CC(CN)=C1
分子式C18H17F4N3O3
分子量399.34
溶解度DMSO : ≥ 130 mg/mL (325.54 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.