PF-05089771 is a Nav1.7 channel blocker with IC50s of 8, 11 and 171 nM for mouse, human and rat Nav1.7, respectively. PF-05089771 exhibits selectivity over a panel of 81 other ion channels, receptors, enzymes and transporters. PF-05089771 blocks spontaneous firing of inherited erythromelalgia (IEM)-derived iPSC sensory neurons in vitro.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO: ≥ 25 mg/mL|
Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7.
Swain NA, et al. J Med Chem. 2017 Aug 24;60(16):7029-7042. PMID: 28682065.
Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release.
Alexandrou AJ, et al. PLoS One. 2016 Apr 6;11(4):e0152405. PMID: 27050761.
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Eleclazine HCl is a novel late Na+ current inhibitor, with IC50 value of 0.7 uM.
Levobupivacaine is a reversible neuronal sodium channel inhibitor.
PF-01247324 is a novel selective and orally bioavailable Nav 1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
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