Examples of the compounds are: (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-(2-(2,2,2- trifluoroethoxy)ethoxy)benzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol; (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-(2-(cyclohex-2-enyloxy)ethoxy)benzyl)phenyl)-6-(hydroxymethyl)...
To determine whether canagliflozin mediates its action solely through OxPhos inhibition, we compared its anti-proliferative activity to that of two specific OxPhos complex-I inhibitors, BAY-87-224347and IACS-01075948. At widely used doses, these agents significantly suppressed OCR in glycolytic rate bi...
In addition to diet and exercise, SGLT2 inhibitors, a class of FDA-approved prescription medications, are used to lower blood sugar levels in people with Type 2 diabetes. Canagliflozin, dapagliflozin, and empagliflozin are examples of drugs that are SGLT2 inhibitors. Single-ingredient formulations ...
SGLT inhibitors were designed to block the eponymous transporter in the proximal (SGLT-2) and distal (SGLT-1) tubule, which is responsible for the reabsorption of glucose filtered by the kidney glomerulus [7]. However, there is a growing body of evidence, that SGLT inhibition exerts its cardi...
(CMCD).2These agents include, but are not limited to, sodium-glucose cotransporter 2 inhibitors (SGLT2is) and glucagon-like peptide-1 receptor agonists (GLP-1RAs) designed initially to lower hyperglycaemia (Figure1).1,...
11 Although examples of carbasugar being reported as a glucose mimetic were limited, those examples have encouraged us to prepare and evaluate carbasugar derivatives as SGLT2 inhibitors (6a–6n).12 Access through your organization Check access to the full text by signing in through your ...
The design and synthesis of the first fluorophore-conjugated SGLT2 inhibitors is described. The mode of linking the fluorophore to the SGLT2 pharmacophore was found to be crucial in achieving optimum potency. Superior potency to phlorizin was provided by examples containing TAMRA, BODIPY, Cy3B and ...