PF-06649298 |
| رقم الكتالوجGC66038 |
PF-06649298 عبارة عن مثبط ناقل سيترات مقترن بالصوديوم (NaCT أو SLC13A5). يتفاعل PF-06649298 على وجه التحديد مع NaCT بقيمة IC50 تبلغ 16.2 μ ؛ M لتثبيط نقل السترات في خلايا الكبد البشرية. يمكن استخدام PF-06649298 للبحث في تنظيم استقلاب الجلوكوز واستقلاب الدهون.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1854061-16-7
Sample solution is provided at 25 µL, 10mM.
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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. |
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