PF-05089771 | Selective Nav1.7 inhibitor
NMR (Conforms)
Available Options
| Size: | Price | Quantity | |
|---|---|---|---|
| 5 mg | $60.00 | ||
| 25 mg | $240.00 |
PF-05089771 (1235403-62-9) is a potent and selective inhibitor of the voltage gated sodium channel 1.7 (Nav1.7).1,3 It is a state-dependent inhibitor with IC50 = 11 nM for the half-inactivated channels and IC50 ~ 10 µM for resting channels.1 Equipotent for human, monkey, dog, and mouse channels but 15x less potent for rat channels. Interacts equally with fast and slow inactivated Nav1.7 channels.2
References/Citations:
- Alexandrou et al. (2016), Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release; PLoS One, 11 e0152405
- Theile et al. (2016), The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels; Mol. Pharmacol., 90 540
- Swain et al. (2017), 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 Na(V)1.7; J. Med. Chem., 60 7029
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
PF-05089771 (1235403-62-9) is a potent and selective inhibitor of the voltage gated sodium channel 1.7 (Nav1.7).1,3 It is a state-dependent inhibitor with IC50 = 11 nM for the half-inactivated channels and IC50 ~ 10 µM for resting channels.1 Equipotent for human, monkey, dog, and mouse channels but 15x less potent for rat channels. Interacts equally with fast and slow inactivated Nav1.7 channels.2
References/Citations:
- Alexandrou et al. (2016), Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release; PLoS One, 11 e0152405
- Theile et al. (2016), The Selective Nav1.7 Inhibitor, PF-05089771, Interacts Equivalently with Fast and Slow Inactivated Nav1.7 Channels; Mol. Pharmacol., 90 540
- Swain et al. (2017), 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 Na(V)1.7; J. Med. Chem., 60 7029
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