PF-06442609 Chemical Properties

Boiling point:

700.0±65.0 °C(Predicted)

Density 

1.37±0.1 g/cm3(Predicted)

storage temp. 

room temp

solubility 

DMSO: 20mg/mL, clear

pka

5.49±0.61(Predicted)

form 

powder

color 

white to beige

PF-06442609 Usage And Synthesis

Uses

PF-06442609 is an orally active γ secretase modulator, with an IC50 of 6 nM for Aβ42. PF-06442609 possesses brain good penetration[1].

Biological Activity

PF-06442609 is a potent γ secretase inhibitor th at produces a robust reduction of brain Aβ42 and Aβ40 in in a guinea pig model. Apparently, PF-06442609 is suitable for rodent model of AD.

References

[1] Martin Pettersson, et al. Design of Pyridopyrazine-1,6-dione γ-Secretase Modulators that Align Potency, MDR Efflux Ratio, and Metabolic Stability. ACS Med Chem Lett. 2015 Apr 3;6(5):596-601. DOI:10.1124/jpet.103.064659