PF-06305591

Product NamePF-06305591
CAS1449473-97-5
MFC15H22N4O
MW274.36
EINECS
MOL File1449473-97-5.mol

Chemical Properties

Boiling point	537.8±50.0 °C(Predicted)
Density	1.176±0.06 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	Solid
pka	11.89±0.10(Predicted)
color	White to off-white

Usage And Synthesis

Uses

PF-06305591 is an effective and highly selective voltage-gated sodium channel NaV1.8 blocker. It has an IC50 value of 15 nM. It has good preclinical in vitro ADME (absorption, distribution, metabolism and excretion) and safety. It also has a number of therapeutic applications and potential therapeutic applications that can be used to treat pain.

Preparation

A solution of tert-butyl [(1S)-3-amino-1-(5-tert-butyl-1H-benzimidazol-2-yl)-2-methyl-3-oxopropyl]carbamate in DCM and React in TFA, then add saturated NaHCO3 aqueous solution, after treatment, PF-06305591 can be obtained.

in vitro

PF-06305591 (compound 9) has a highly attractive profile with respect to NaV selectivity, hERG activity, passive permeability and in vitro metabolic stability.

< /p>

in vivo

PF-06305591 (compound 9) has good rat bioavailability. It offers the possibility of investigating higher IC ₅₀ multiples of Nav1.8 blockade in the clinic, and therefore a more Thorough evaluation of the role of NaV1.8 in the treatment of pain.