IC50: 408 nM (citrate uptake in HEKNaCT), 16.2 μM (citrate uptake in Human Heps), 4.5 μM (citrate uptake in Mouse Heps), ＞100 μM (citrate uptake in HEKNaCD1), ＞100 μM (citrate uptake in HEKNaCD3)[1][2]
PF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 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[1][2].
PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells[1].
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 IC50s 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 high fat diet (HFD) mice[2].
| Animal Model: | Mice with high fat diet (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. |