PF-06305591 |
| カタログ番号GC31095 |
PF-06305591 は、15 nM の IC50 を持つ、強力で高度に選択的な電位依存性ナトリウム チャネル NaV1.8 ブロッカーです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1449473-97-5
Sample solution is provided at 25 µL, 10mM.
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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].
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.
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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