PF-06649298
Based on 1 publication(s) in Google Scholar
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.
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- Pureté: 98.32%
- CAS No.: 1854061-16-7
- Formule: C16H22O5
- Masse moléculaire:294.34
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PF-06649298
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Activité biologique
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]
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
>100 μM
Compound: 1a; PF-06649298
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Inhibition of NaDC1 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
Inhibition of NaDC1 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
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[PMID: 26734723] |
| HEK293 | IC50 |
>100 μM
Compound: 1a; PF-06649298
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Inhibition of NaDC3 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
Inhibition of NaDC3 (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
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[PMID: 26734723] |
| HEK293 | IC50 |
0.41 μM
Compound: 1a; PF-06649298
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Inhibition of NaCT (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
Inhibition of NaCT (unknown origin) expressed in HEK293 cells assessed as inhibition of [14C]citrate uptake by microbeta plate reader analysis
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[PMID: 26734723] |
| HEK-293T | IC50 |
0.41 μM
Compound: 2; PF-06649298
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Inhibition of citrate uptake expressed in HEK293T
Inhibition of citrate uptake expressed in HEK293T
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[PMID: 37428122] |
| Hepatocyte | IC50 |
16.2 μM
Compound: 1a; PF-06649298
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Inhibition of NaCT in human hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method
Inhibition of NaCT in human hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method
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[PMID: 26734723] |
PF-06649298 (0-100 μM; 30 min) inhibits citrate uptaken in cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK-293 cells expressing NaCT, NaDC1 or NaDC3, human hepatocytes and mouse epatocytes
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Concentration:0-100 μM
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Incubation Time:30 min
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice with high fat diet (HFD) administration[2]
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Dosage:250 mg/kg
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Administration:Oral gavage; 250mg/kg twice a day; for 21 days
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Result:Decreased plasma glucose, hepatic triglycerides, diacylglycerides, and acyl-carnitines concentration of livers in HFD mice. Totally reversed glucose intolerance of HFD mice.
Chemical Information
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CAS No. 1854061-16-7
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Appearance Solid
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Masse moléculaire 294.34
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Formule C16H22O5
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Color Off-white to light yellow
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SMILES
O=C(O)[C@@](O)(CCC1=CC=C(C(C)(C)C)C=C1)CC(O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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bioRxiv
2025 Jun 19:2025.06.17.660213. PMID: 40611907
Solvant et solubilité
DMSO : 100 mg/mL (339.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Huard K, et al. Optimization of a Dicarboxylic Series for in Vivo Inhibition of Citrate Transport by the Solute Carrier 13 (SLC13) Family. J Med Chem. 2016 Feb 11;59(3):1165-75. [Content Brief]
[2]. Huard K, et al. Discovery and characterization of novel inhibitors of the sodium-coupled citrate transporter (NaCT or SLC13A5). Sci Rep. 2015 Dec 1;5:17391. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.3974 mL | 16.9872 mL | 33.9743 mL | 84.9358 mL |
| 5 mM | 0.6795 mL | 3.3974 mL | 6.7949 mL | 16.9872 mL | |
| 10 mM | 0.3397 mL | 1.6987 mL | 3.3974 mL | 8.4936 mL | |
| 15 mM | 0.2265 mL | 1.1325 mL | 2.2650 mL | 5.6624 mL | |
| 20 mM | 0.1699 mL | 0.8494 mL | 1.6987 mL | 4.2468 mL | |
| 25 mM | 0.1359 mL | 0.6795 mL | 1.3590 mL | 3.3974 mL | |
| 30 mM | 0.1132 mL | 0.5662 mL | 1.1325 mL | 2.8312 mL | |
| 40 mM | 0.0849 mL | 0.4247 mL | 0.8494 mL | 2.1234 mL | |
| 50 mM | 0.0679 mL | 0.3397 mL | 0.6795 mL | 1.6987 mL | |
| 60 mM | 0.0566 mL | 0.2831 mL | 0.5662 mL | 1.4156 mL | |
| 80 mM | 0.0425 mL | 0.2123 mL | 0.4247 mL | 1.0617 mL | |
| 100 mM | 0.0340 mL | 0.1699 mL | 0.3397 mL | 0.8494 mL |
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