PF-06649298

PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 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 for the research of regulating glucose metabolism and lipid metabolism In Vitro PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell 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. In Vivo PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of high fat diet (HFD) mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice with high fat diet (HFD) administrationDosage: 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. Form:Solid IC50& Target:IC50: 408 nM (citrate uptake in HEK NaCT ), 16.2 μM (citrate uptake in Human Heps), 4.5 μM (citrate uptake in Mouse Heps), ＞100 μM (citrate uptake in HEK NaCD1 ), ＞100 μM (citrate uptake in HEK NaCD3 )

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