PF-06761281
Based on 1 publication(s) in Google Scholar
PF-06761281 (Compound 4a) is a potent, orally active, partial selective sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor with IC50 values of 0.51, 13.2 and 14.1 µM against HEKNaCT, HEKNaDC1 and HEKNaDC3, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.52%
- No. CAS: 1854061-19-0
- Fòrmula: C13H17NO6
- Peso molecular:283.28
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Almacenamiento:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PF-06761281
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Actividad biológica
Descripciòn
IC50 & Target
IC50: 0.51 µM (HEKNaCT), 13.2 µM (HEKNaDC1), 14.1 µM (HEKNaDC3)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.51 μM
Compound: 4a; PF-06761281
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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] |
| HEK293 | IC50 |
13.2 μM
Compound: 4a; PF-06761281
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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 |
14.1 μM
Compound: 4a; PF-06761281
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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] |
| Hepatocyte | IC50 |
0.12 μM
Compound: 4a; PF-06761281
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Inhibition of NaCT in rat hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method
Inhibition of NaCT in rat hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method
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[PMID: 26734723] |
| Hepatocyte | IC50 |
0.21 μM
Compound: 4a; PF-06761281
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Inhibition of NaCT in mouse hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method
Inhibition of NaCT in mouse hepatocytes assessed as [14C]-citrate uptake after 30 mins by scintillation counting method
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[PMID: 26734723] |
| Hepatocyte | IC50 |
0.74 μM
Compound: 4a; PF-06761281
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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] |
In Vitro
PF-06761281 (Compound 4a) inhibits citrate uptake with IC50 values of 0.12, 0.21 and 0.74 µM in rat, mouse and human Heps[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1854061-19-0
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Appearance Solid
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Peso molecular 283.28
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Fòrmula C13H17NO6
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Color Off-white to light yellow
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SMILES
O=C(O)[C@](CCC1=CC(C)=CN=C1OC)(O)CC(O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nat Commun
SLC13A3 is a major effector downstream of activated β-catenin in liver cancer pathogenesis. [Abstract]2024 Aug 30;15(1):7522. PMID: 39215042
Solvente y solubilidad
In Vitro:
DMSO : 100 mg/mL (353.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (176.50 mM)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (8.83 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (8.83 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 (sealed storage, away from moisture). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 3.5301 mL | 17.6504 mL | 35.3008 mL | 88.2519 mL |
| 5 mM | 0.7060 mL | 3.5301 mL | 7.0602 mL | 17.6504 mL | |
| 10 mM | 0.3530 mL | 1.7650 mL | 3.5301 mL | 8.8252 mL | |
| 15 mM | 0.2353 mL | 1.1767 mL | 2.3534 mL | 5.8835 mL | |
| 20 mM | 0.1765 mL | 0.8825 mL | 1.7650 mL | 4.4126 mL | |
| 25 mM | 0.1412 mL | 0.7060 mL | 1.4120 mL | 3.5301 mL | |
| 30 mM | 0.1177 mL | 0.5883 mL | 1.1767 mL | 2.9417 mL | |
| 40 mM | 0.0883 mL | 0.4413 mL | 0.8825 mL | 2.2063 mL | |
| 50 mM | 0.0706 mL | 0.3530 mL | 0.7060 mL | 1.7650 mL | |
| 60 mM | 0.0588 mL | 0.2942 mL | 0.5883 mL | 1.4709 mL | |
| 80 mM | 0.0441 mL | 0.2206 mL | 0.4413 mL | 1.1031 mL | |
| 100 mM | 0.0353 mL | 0.1765 mL | 0.3530 mL | 0.8825 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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