PF-06649298|cas:1854061-16-7|西域试剂

PF-06649298,99.51%

产品编号：Bellancom-120103| CAS NO：1854061-16-7| 分子式：C₁₆H₂₂O₅| 分子量：294.34

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货号	价格	库存与货期
Bellancom-120103	￥4500.00	杭州北京（现货）
Bellancom-120103	￥8000.00	杭州北京（现货）
Bellancom-120103	￥16500.00	杭州北京（现货）
Bellancom-120103	￥25500.00	杭州北京（现货）
Bellancom-120103	￥38000.00	杭州北京（现货）

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PF-06649298

产品介绍

PF-06649298 是一个 sodium-coupled citrate transporter (NaCT or SLC13A5) 抑制剂。PF-06649298 在人类肝细胞中与 NaCT 结合从而抑制柠檬酸盐运输，其 IC₅₀ 值为 16.2 μM。PF-06649298 可用于调节糖代谢以及脂代谢的研究。

生物活性

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.

体外研究

PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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.

体内研究
(In Vivo)

PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of high fat diet (HFD) mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice with high fat diet (HFD) administration
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.

体内研究

PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of high fat diet (HFD) mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice with high fat diet (HFD) administration
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.

体内研究

PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of high fat diet (HFD) mice.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice with high fat diet (HFD) administration
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.