Saxagliptin

Benzyloxycarbonyl-Val-Ala-Asp (OMe) fluoromethylketone (Z-VAD-FMK) was purchased from Medical and Biological Laboratories (Nagoya, Japan). 1G244 was purchased from AK Scientific (Union city, CA). Alogliptin was purchased from ChemScene (Monmouth Junction, NJ). Linagliptin was purchased from BioVision (Milpitas, CA). Sitagliptin and Bortezomib were purchased from Santa Cruz Biotechnology (Santa Cruz, CA). Vildagliptin was purchased from LKT Laboratories (St. Paul, MN). Saxagliptin was purchased from Adooq Bioscience (Irvine, CA).

HL-1 cells were treated with indicated (in respective Figures and Figure legends) concentrations of saxagliptin or sitagliptin (Adooq Bioscience, CA, United States, dissolved in DMSO, final concentration of DMSO – 0.01% [v/v]) for indicated time periods.

Saxagliptin, trelagliptin, and gemigliptin (Figure 1) were purchased from AdooQ Bioscience (>98%, Irvine, CA, USA); linagliptin and 5-hydroxySaxagliptin from Toronto Research Chemicals (Toronto, Canada); ammonium acetate (99.99%), β-nicotinamide adenine dinucleotide phosphate sodium salt hydrate (NADP⁺), dimethyl sulfoxide (DMSO, >99.7%), glucose-6-phosphate (G6P), glucose-6-phosphate dehydrogenase (G6PD), L-cysteine, magnesium chloride, reduced glutathione (GSH, ≥99%), 3′-phosphoadenosine-5′-phosphosulfate (PAPS), potassium phosphate, uridine diphosphate glucuronic acid (UDPGA, >98%), and vildagliptin from Sigma-Aldrich (St. Louis, MO, USA); and rat liver microsomes (RLM, R1000) from XenoTech (Lenexa, KS, USA). All solvents were LC-MS grade from Fisher Scientific (Pittsburgh, PA, USA).