PF-06649298

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PF-06649298

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1854061-16-7

包装与价格：

包装	价格(元)
10mg	询价
25mg	询价
50mg	询价
100mg	询价

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。

Cas No.

1854061-16-7

分子式

C₁₆H₂₂O₅

分子量

294.34

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

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)^[1]^[2]

PF-06649298 is asodium-coupled citrate transporter (NaCT or SLC13A5)inhibitor. PF-06649298 specifically interacts with NaCT with anIC₅₀value 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.