BI01383298 is a potent, non-competitive, irreversible inhibitor of the human Na+-coupled citrate transporter (NaCT/SLC13A5/mINDY).1,2 IC50 = 49 nM in the presence of Li+ with preincubation and 118 nM without Li+. BI01393298 is inactive in mouse NaCT for citrate transport. NaCT delivers citrate, a key metabolite and regulator of multiple biochemical pathways, from the blood to hepatocytes and neurons. Reduced expression of NaCT has been linked to longevity and increased expression has been linked to type 2 diabetes and non-alcoholic fatty liver disease. BI01383298 also blocked transport of arginine, dimethylarginine, and L-homoarginine in both human and mouse NaCT.2
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