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PF-06761281

Name: PF-06761281
Brand: TargetMol
SKU: T60547
Rating: 4.5 (1 reviews)

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Catalog No. T60547Cas No. 1854061-19-0

Alias PF06761281

PF-06761281 (Compound 4a) is a potent and partially selective sodium-coupled citrate transporter protein (NaCT/SLC13A5) inhibitor with IC50 values of 0.51, 13.2, and 14.1 µM for NaCT, NaDC, and NaDC, respectively, and has the advantage of being orally active, reducing hepatic and renal uptake of citrate and plasma glucose concentration for metabolic diseases.

PF-06761281

🥰Excellent

Catalog No. T60547Alias PF06761281Cas No. 1854061-19-0

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Appearance:Viscous

Color:Transparent

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Product Introduction

Bioactivity

Description	PF-06761281 (Compound 4a) is a potent and partially selective sodium-coupled citrate transporter protein (NaCT/SLC13A5) inhibitor with IC50 values of 0.51, 13.2, and 14.1 µM for NaCT, NaDC, and NaDC, respectively, and has the advantage of being orally active, reducing hepatic and renal uptake of citrate and plasma glucose concentration for metabolic diseases.
Targets&IC50	Selectivity over NaDC1/NaDC3:~13 μM, HEK293 cells:0.51 μM
In vitro	PF-06761281 is a NaCT inhibitor with an IC₅₀ of 0.51 μM in HEK293 cells, and 0.74, 0.21, and 0.12 μM in human, mouse, and rat hepatocytes, respectively. PF-06761281 shows good selectivity over NaDC1/NaDC3 (IC₅₀ ~13 μM). Water solubility is 24 mM (pH 6.5), permeability is low (P_app = 0.3×10⁻⁶ cm/s), and hepatocyte clearance is <7 μL/min/10⁶ cells[1].
Synonyms	PF06761281

Chemical Properties

Molecular Weight	283.28
Formula	C₁₃H₁₇NO₆
Cas No.	1854061-19-0
Smiles	C(C[C@@](CC(O)=O)(C(O)=O)O)C1=C(OC)N=CC(C)=C1

Storage & Solubility Information

Storage

keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: 40 mg/mL (141.2 mM), Sonication is recommended.

Solution Preparation Table

H2O

	1mg	5mg	10mg	50mg
1 mM	3.5301 mL	17.6504 mL	35.3008 mL	176.5038 mL
5 mM	0.7060 mL	3.5301 mL	7.0602 mL	35.3008 mL
10 mM	0.3530 mL	1.7650 mL	3.5301 mL	17.6504 mL
20 mM	0.1765 mL	0.8825 mL	1.7650 mL	8.8252 mL
50 mM	0.0706 mL	0.3530 mL	0.7060 mL	3.5301 mL
100 mM	0.0353 mL	0.1765 mL	0.3530 mL	1.7650 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

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