2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. PF-06761281

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.

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

PF-06761281

PF-06761281 Chemical Structure

CAS No. : 1854061-19-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

PF-06761281 Related Antibodies

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1 Publications Citing Use of MCE PF-06761281

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1].

IC50 & Target

IC50: 0.51 µM (HEKNaCT), 13.2 µM (HEKNaDC1), 14.1 µM (HEKNaDC3)[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.51 μM
Compound: 4a; PF-06761281
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
[PMID: 26734723]
HEK293 IC50
13.2 μM
Compound: 4a; PF-06761281
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
[PMID: 26734723]
HEK293 IC50
14.1 μM
Compound: 4a; PF-06761281
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
[PMID: 26734723]
Hepatocyte IC50
0.12 μM
Compound: 4a; PF-06761281
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
[PMID: 26734723]
Hepatocyte IC50
0.21 μM
Compound: 4a; PF-06761281
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
[PMID: 26734723]
Hepatocyte IC50
0.74 μM
Compound: 4a; PF-06761281
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
[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.

PF-06761281 Related Antibodies
Molecular Weight

283.28

Formula

C13H17NO6
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(O)[C@](CCC1=CC(C)=CN=C1OC)(O)CC(O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.5301 mL 17.6504 mL 35.3008 mL
5 mM 0.7060 mL 3.5301 mL 7.0602 mL
View the 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.

* 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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.

  • Protocol 1

    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.
  • Protocol 2

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.52%

SDS (479 KB)

COA (249 KB) HNMR (145 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References

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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PF-06761281 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-067612811854061-19-0PF06761281PF 06761281Sodium ChannelNa channelsNa+ channelsSLC13A5NaCTcitrate uptakeHeporally activeInhibitorinhibitorinhibit

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