In Vitro and In Vivo Correlation of Hepatic Fraction of Metabolism by P450 in Dogs was written by Zhou, Xin;Hui, Yu-Hua;Hudson, Loyd;Katyayan, Kishore K.;Mohutsky, Michael A.;Hao, Junliang;Schober, Douglas A.;Hembre, Erik J.. And the article was included in Journal of Pharmaceutical Sciences (Philadelphia, PA, United States) in 2019.Product Details of 1614-12-6 This article mentions the following:
1-Aminobenzotriazole (ABT) has been widely used as a nonspecific mechanism-based inhibitor of cytochrome P 450 enzymes. It is extensively used in preclin. studies to determine the relative contribution of oxidative metabolism mediated by P 450 in vitro and in vivo. The aim of present study was to understand the translation of fraction metabolized by P 450 in dog hepatocytes to in vivo using ABT, for canagliflozin, known to be cleared by P 450-mediated oxidation and UDP-glucuronosyltransferases-mediated glucuronidation, and three drug discovery project compounds mainly cleared by hepatic metabolism In a dog hepatocyte, intrinsic clearance assay with and without preincubation of ABT, three Lilly (LY) compounds exhibited a wide range of fraction metabolized by P 450. Subsequent metabolite profiling in dog hepatocytes demonstrated a combination of metabolism by P 450 and UDP-glucuronosyltransferases. In vivo, dogs were pretreated with 50 mg/kg ABT or vehicle at 2 h before i.v. administration of canagliflozin and LY compounds The areas under the concentration-time curve (AUC) were compared for the ABT-pretreated and vehicle-pretreated groups. The measured AUCABT/AUCveh ratios were correlated to fraction of metabolism by P 450 in dog hepatocytes, suggesting that in vitro ABT inhibition in hepatocytes is useful to rank order compounds for in vivo fraction of metabolism assessment. In the experiment, the researchers used many compounds, for example, 1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6Product Details of 1614-12-6).
1H-Benzo[d][1,2,3]triazol-1-amine (cas: 1614-12-6) belongs to triazole derivatives. The many free lone pairs in triazoles make them useful as coordination compounds, although not typically as haptic ligands. Triazoles are compounds with a vast spectrum of applications, varying from materials (polymers), agricultural chemicals, pharmaceuticals, photoactive chemicals and dyes.Product Details of 1614-12-6
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics