PF-06471553 Chemical Properties

Boiling point:

728.7±70.0 °C(Predicted)

Density 

1.46±0.1 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

DMSO : ≥ 150 mg/mL (320.83 mM)

form 

Solid

pka

6.75±0.20(Predicted)

color 

White to off-white

PF-06471553 Usage And Synthesis

Description

PF-06471553 is a potent and selective Monoacylglycerol acyltransferase 3 (MGAT3) inhibitor. PF-06471553 selectively inhibits MGAT3 with high in vitro potency and cell efficacy. In the presence of a combination of diacylglycerol acyltransferases 1 and 2 (DGAT1 and DGAT2) inhibitors, an oral administration of PF-06471553 exhibited inhibition of the incorporation of deuterium-labeled glycerol into TAG in mouse model. Inhibition of triacylglycerol (TAG) biosynthetic enzymes has been suggested as a promising strategy to treat insulin resistance, diabetes, dyslipidemia, and hepatic steatosis.

Uses

PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.

in vivo

References

[1] Huard K, et al. Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3. J Med Chem. 2015 Sep 24;58(18):7164-72. DOI:10.1021/acs.jmedchem.5b01008