PF-06305591dihydrate是一种有效的、高选择性的电压门控钠通道NaV1.8的阻断剂，其IC50值为15nM。具有良好的临床前体外ADME(吸收、分布、代谢和排泄)和安全性。
PF-06305591 dihydrate is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile[1].
PF-06305591 (compound 9) has a highly attractive profile with respect to NaV selectivity, hERG activity, passive permeability and in vitro metabolic stability[1].
PF-06305591 (compound 9) has good rat bioavailability. PF-06305591 offers the possibility of investigating higher IC50 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[1].
[1]. Brown AD, et al. The discovery and optimization of benzimidazoles as selective NaV1.8 blockers for the treatment of pain. Bioorg Med Chem. 2019 Jan 1;27(1):230-239.
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