PF-05089771 (tosylate) |
| Catalog No.GC18947 |
PF-05089771 (tosilato) es un inhibidor de arilsulfonamida Nav1.7 potente, activo por vía oral y selectivo, con valores IC50 de 11 nM, 12 nM, 13 nM, 171 nM y 8 nM para hNav1.7, cynNav1.7, dogNav1.7 ,ratNav1.7 y musNav1.7, respectivamente.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1430806-04-4
Sample solution is provided at 25 µL, 10mM.
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PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50s = 11, 16, 33, and 20 nM for 5N11S, 5A11L, 5A11S, and 5A11L Nav1.7 splice variants, respectively). It is selective for Nav1.7 over Nav1.1-1.6 and 1.8 channels (IC50s = 0.11-25 μM), L-type calcium, and KvLQT and hERG potassium channels (IC50s =>10 μM), as well as human and cynomolgus monkey TRPV1 receptors (IC50s = 10 and 20 μM, respectively). PF-05089771 is also 1,000-fold selective for half-inactivated over resting Nav1.7 channels, and mutation of the domain IV voltage-sensor domain (VSD4) reduces PF-05089771 potency by approximately 100-fold.
Review for PF-05089771 (tosylate)
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
Review for PF-05089771 (tosylate)
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