PF-06649298 is an inhibitor of sodium-coupled citrate transporter which specifically interacts with NaCT with an IC 50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used in regulating metabolism of glucose and metabolism of lipid [1] [2].

PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells [2]. Cell Viability Assay [1] Cell Line: HEK-293 cells expressing NaCT, NaDC1 or NaDC3, human hepatocytes and mouse epatocytes Concentration: 0-100 μM Incubation Time: 30 min Result: Showed a selectivity for NaCT over the dicarboxylate transporters NaDC1 and NaDC3. Inhibited citrate uptake in HEK-293 cells expressing NaCT, NaDC1 or NaDC3, human hepatocytes and mouse epatocytes with IC 50 s of 408 nM, ＞100 μM, ＞100 μM, 16.2 μM and 4.5 μM, respectively.

PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of HFD mice [1]. Animal Model: Mice with HFD administration [2] Dosage: 250 mg/kg Administration: Oral gavage; 250mg/kg twice a day; for 21 days Result: Decreased plasma glucose, hepatic triglycerides, diacylglycerides, and acyl-carnitines concentration of livers in HFD mice. Totally reversed glucose intolerance of HFD mice.