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.
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.
PF-06305591 is a potent and highly selective sodium channel Nav1.8 inhibitor.', 'PF-06305591 is safe and has acceptable absorption, distribution, metabolism, and elimination (ADME) properties.
PF-06305591 (compound 9) has a highly attractive profile with respect to NaV selectivity, hERG activity, passive permeability and in vitro metabolic stability.
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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.
