| Description |
PF-06305591 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].
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| Related Catalog |
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| Target |
IC50: 15 nM (NaV1.8)[1].
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| 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[1].
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| In Vivo |
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].
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| References |
[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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