ttx-r

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-typ

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV. It shows a slow onset of the block that is depolarization and concentration-dependent.

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

Oe-9000 is a blocker of voltage-gated Na(+) currents in neurons. It reversibly reduces rapidly activating and inactivating TTX-sensitive (TTX-S) Na(+) currents as well as slowly activating and inactivating tetrodotoxin-resistant (TTX-R) Na(+) currents at

Jingzhaotoxin-II, a neurotoxin composed of 32 amino acid residues featuring two acidic and two basic residues, selectively inhibits voltage-gated sodium channels (VGSC), notably slowing the rapid inactivation of TTX-resistant (TTX-R) VGSC in cardiac myocytes, with an IC50 of 0.26 μM [1].

Jingzhaotoxin-34, a 35-residue neurotoxic polypeptide, selectively inhibits tetrodotoxin-sensitive (TTX-S) sodium currents in rat dorsal root ganglion neurons with an IC50 of approximately 85 nM and exerts negligible influence on tetrodotoxin-resistant (TTX-R) sodium currents [1].