PF-06761281 Chemical Properties

Boiling point:

469.7±45.0 °C(Predicted)

Density 

1.358±0.06 g/cm3(Predicted)

storage temp. 

-20°C

form 

powder

pka

3.37±0.28(Predicted)

color 

white to beige

Safety Information

RIDADR 

UN 2811 6.1 / PGIII

PF-06761281 Usage And Synthesis

Uses

PF-06761281 has been used as a SLC13A family inhibitor, in rats to determine its unbound partition coefficient (Kpuu), to estimate its potency as a drug.

General Description

PF-06761281 is a small, polar dicarboxylate compound. Its structure is similar to citrate, which is the endogenous substrate of Na⁺-citrate cotransporter (NaCT). It is a novel, potent inhibitor of SLC13a2/3/5 (solute channel) family, along with selectivity for NaCT.

Biochem/physiol Actions

PF-06761281 is an inhibitor of the sodium-coupled citrate transporter (NaCT or SLC13A5), which may be a target for tretment and prevention of metabolic disorders. The SLC13 transporters SLC13A2 (NaDC1), SLC13A3 (NaDC3), and SLC13A5 (NaCT) co-transport di- and tricarboxylates with multiple sodium ions into cells. PF-06761281 inhibits citrate uptake with an IC50 of 740 nM for NaCT in human hepatocytes. PF-06761281 has >25-fold in vitro selectivity for NaCT over NaDC1 and NaDC3 and was inactive in a selectivity panel of 65 targets.