| 产品介绍 |
PF-05089771 is a voltage-gated sodium channel 1.7 (Nav1.7) blocker (IC50: 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 (IC50: 0.11-25 μM), L-type calcium, and KvLQT and hERG potassium channels (IC50: ≥10 μM), as well as human and cynomolgus monkey TRPV1 receptors (IC50: 10/20 μM). 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.
|
