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PF-06761281

🥰Excellent
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

PF-06761281

🥰Excellent
Catalog No. T60547Alias PF06761281Cas No. 1854061-19-0
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.
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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
HEK293 cells:0.51 μM, Selectivity over NaDC1/NaDC3:~13 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].
AliasPF06761281
Chemical Properties
Molecular Weight283.28
FormulaC13H17NO6
Cas No.1854061-19-0
SmilesC(C[C@@](CC(O)=O)(C(O)=O)O)C1=C(OC)N=CC(C)=C1
Storage & Solubility Information
Storagekeep 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
1mg5mg10mg50mg
1 mM3.5301 mL17.6504 mL35.3008 mL176.5038 mL
5 mM0.7060 mL3.5301 mL7.0602 mL35.3008 mL
10 mM0.3530 mL1.7650 mL3.5301 mL17.6504 mL
20 mM0.1765 mL0.8825 mL1.7650 mL8.8252 mL
50 mM0.0706 mL0.3530 mL0.7060 mL3.5301 mL
100 mM0.0353 mL0.1765 mL0.3530 mL1.7650 mL

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TargetMol | Animal experimentsFor example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSOTargetMol | reagent (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH2OTargetMol | reagent mix well and clarify
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