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PF-06649298

Catalog No. T60629 CAS 1854061-16-7

PF-06649298 is an inhibitor of sodium-coupled citrate transporter which 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 in regulating metabolism of glucose and metabolism of lipid [1] [2].

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PF-06649298, CAS 1854061-16-7

Pack Size	Availability	Price/USD
25 mg	6-8 weeks	$ 1,620.00
50 mg	6-8 weeks	$ 2,110.00
1 mL * 10 mM (in DMSO)	6-8 weeks	$ 397.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

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Description	PF-06649298 is an inhibitor of sodium-coupled citrate transporter which 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 in regulating metabolism of glucose and metabolism of lipid [1] [2].
In vitro	PF-06649298, at concentrations ranging from 0 to 100 μM over a 30-minute incubation period, demonstrates selective inhibition of citrate uptake, particularly targeting the NaCT transporter over dicarboxylate transporters NaDC1 and NaDC3. This effect is observed across HEK-293 cells (expressing NaCT, NaDC1, or NaDC3), human hepatocytes, and mouse hepatocytes, with IC50 values of 408 nM, >100 μM, >100 μM, 16.2 μM, and 4.5 μM, respectively. These findings underscore the compound's specific action on citrate transport mechanisms within the tested cell types.
In vivo	PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) effectively mitigates glucose intolerance in mice subjected to a high-fat diet (HFD) [1]. Utilizing an animal model of HFD-induced mice [2], the study administered PF-06649298 orally at a dosage of 250 mg/kg twice daily over a period of 21 days. The outcomes demonstrated a significant reduction in plasma glucose, hepatic triglycerides, diacylglycerides, and acyl-carnitines levels in the livers of HFD mice, ultimately reversing their glucose intolerance.

Molecular Weight	294.34
Formula	C16H22O5
CAS No.	1854061-16-7

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

PF-06649298 1854061-16-7 inhibitor inhibit

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