Description | PF-06305591 is an effective and selective blocker of voltage-gated sodium channel NaV1.8 (IC50 = 15 nM). |
In vitro | PF-06305591表现出高度的NaV选择性、被动渗透性、hERG活性以及体外代谢稳定性[1]。 |
In vivo | PF-06305591在大鼠中展现出良好的生物利用度,可用于疼痛治疗研究[1]。 |
Target activity | Nav1.8:15 nM |
Synonyms | PF-6305591 |
molecular weight | 274.36 |
Molecular formula | C15H22N4O |
CAS | 1449473-97-5 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility | DMSO: 45 mg/mL (164.02 mM), Sonication is recommended. |
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. |