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PF-06649298 

Cat. No.: HY-120103
Handling Instructions

PF-06649298 is a sodium-coupled citrate transporter 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.

For research use only. We do not sell to patients.

PF-06649298 Chemical Structure

PF-06649298 Chemical Structure

CAS No. : 1854061-16-7

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Description

PF-06649298 is a sodium-coupled citrate transporter 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].

IC50 & Target

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]

In Vitro

PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells[2].

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

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.
In Vivo

PF-06649298 (250 mg/kg; p.o. twice a day; for 21 days) reverses glucose intolerance of HFD mice[1].

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

Animal Model: Mice with 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.
Molecular Weight

294.34

Formula

C16H22O5

CAS No.
SMILES

O=C(O)[[email protected]@](O)(CCC1=CC=C(C(C)(C)C)C=C1)CC(O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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PF-06649298
Cat. No.:
HY-120103
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