PAT-1251 is a Potent, Selective, and orally Efficacious Inhibitors of the Copper-Dependent Amine Oxidase, Lysyl Oxidase-Like 2 (LOXL2). PAT-1251 showed LOXL2 IC50 = 0.074 μM; > 400-fold selective over LOX. PAT-1251 was also potent against mouse, rat, and dog LOXL2 (average IC50 of 0.10, 0.12, and 0.16 μM, respectively) . PAT-1251 also exhibits a reasonable CYP450 inhibition profile, with measured IC50 of 1.8, 1.7, 2.4, 12, and 30 μM versus 1A2, 2C9, 2C19, 2D6, and 3A4, respectively. References: Rowbottom MW, Bain G, Calderon I, Lasof T, Lonergan D, Lai A, Huang F, Darlington J, Prodanovich P, Santini AM, King CD, Goulet L, Shannon KE, Ma GL, Nguyen K, MacKenna DA, Evans JF, Hutchinson JH. 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 15. doi: 10.1021/acs.jmedchem.7b00345. [Epub ahead of print] PubMed PMID: 28471663.
纯度:≥98%
CAS:2007885-39-2