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Chemical Structure : PF-05089771
CAS No.: 1235403-62-9
Catalog No.: PC-63166Not For Human Use, Lab Use Only.
PF-05089771 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, >1,000-fold selectivity over Nav1.3, 1.4 and Nav1.5, 1.8.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $158 | In stock | |
| 10 mg | $258 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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PF-05089771 is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 11 nM, >1,000-fold selectivity over Nav1.3, 1.4 and Nav1.5, 1.8.
PF-05089771 interacts with the voltage-sensor domain (VSD) of domain IV, blocks all Nav1.7 splice variants with similar potency (5N11L, 5A11S, 5A11L and 5N11S, IC50s=11=33 nM).
PF-05089771 displays high selectivity over L-type calcium channels, KvLQT and hERG potassium channels.
PF-05089771 demonstrates in vivo efficacy in a mouse capsaicin-induced neurogenic flare model.
| M.Wt | 500.344 | |
| Formula | C18H12Cl2FN5O3S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-[2-(5-amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-(1,3-thiazol-4-yl)benzenesulfonamide |
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1. Swain NA, et al. J Med Chem. 2017 Aug 24;60(16):7029-7042.
2. Theile JW, et al. Mol Pharmacol. 2016 Nov;90(5):540-548.
3. Alexandrou AJ, et al. PLoS One. 2016 Apr 6;11(4):e0152405.
4. Chernov-Rogan T, et al. Proc Natl Acad Sci U S A. 2018 Jan 23;115(4):E792-E801.
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