Functional characterization and comparison of human and mouse organic anion transporter 1 as drugs and pesticides uptake carrier was written by Floerl, Saskia;Kuehne, Annett;Hagos, Yohannes. And the article was included in European Journal of Pharmaceutical Sciences in 2022.COA of Formula: C23H28ClN3O5S This article mentions the following:
The organic anion transporter 1 (OAT1) is mainly expressed in proximal tubule cells, where it mediates the renal uptake of endogenous and exogenous compounds Thereby, it has enormous clin. relevance particularly in drug-drug interactions. The aim of the present in vitro study was to elucidate potential species dependent disparity of human and mouse OAT1 in handling of structural diverse drugs and pesticides. A basic functional comparison of the two transporters showed a similar time-dependent uptake of the substrate para-aminohippuric acid (PAH), the affinity (Km) was 94μM for hOAT1 and 32μM for mOat1. Inhibition experiments for hOAT1 and mOat1 provided IC50 values for glibenclamide of 5.1 and 6.4μM and for probenecid of 31 and 11μM. Than the interaction of hOAT1 and mOat1 with 23 drugs and 13 pesticides was examined Three pesticides and thirteen drugs showed high inhibitory potency of 50% or more to both transporters. Furthermore, we identified rosiglitazone as a differential active inhibitor, with stronger inhibitory properties (IC50) to mOat1 (7.7μM) than to hOAT1 (31μM), and olmesartan with the most pronounced difference: The IC50 of hOAT1 (0.40μM) was 48-fold lower than of mOat1 (19μM). In conclusion, we found a strong correlation for the inhibitory effects of most drugs and pesticides on human and mouse OAT1. But the example of olmesartan shows that species differences have to be considered when extrapolating data from mouse to human. In the experiment, the researchers used many compounds, for example, 5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8COA of Formula: C23H28ClN3O5S).
5-Chloro-N-(4-(N-(cyclohexylcarbamoyl)sulfamoyl)phenethyl)-2-methoxybenzamide (cas: 10238-21-8) belongs to amides. Amides can be viewed as a derivative of a carboxylic acid RC(=O)OH with the hydroxyl group –OH replaced by an amine group −NR′R″; or, equivalently, an acyl (alkanoyl) group RC(=O)− joined to an amine group. Amides can be freed from solvent or water by drying below their melting points. These purifications can also be used for sulfonamides and acid hydrazides.COA of Formula: C23H28ClN3O5S
Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics