Description

ProTx II is a selective blocker of Nav1.7 sodium channels with an IC50 of 0.3 nM, and is at least 100-fold selective for Nav1.7 over other sodium channel subtypes. ProTx-II inhibits sodium channels by decreasing channel conductance and shifting activation to more positive potentials and blocks action potential propagation in nociceptors[1][2].—Neuroscience-Neuromodulation–C168H250N46O41S8—-[1]Tanaka K, et al. Antihyperalgesic effects of ProTx-II, a Nav1.7 antagonist, and A803467, a Nav1.8 antagonist, in diabetic mice. J Exp Pharmacol. 2015 Jun 24;7:11-6.|[2]Schmalhofer WA, et al. ProTx-II, a selective inhibitor of NaV1.7 sodium channels, blocks action potential propagation in nociceptors. Mol Pharmacol. 2008 Nov;74(5):1476-84.–484598-36-9–3826.59—-O=C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCC(O)=O)C(NCC(N[C@@H](CCSC)C(N[C@H]1C(C)C)=O)=O)=O)=O)NC2=O)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCCN)C(N[C@@H](CC3=CNC4=CC=CC=C34)C(N[C@@H](CCSC)C(N[C@@H](CC5=CNC6=CC=CC=C56)C(N[C@@H]([C@H](O)C)C(N[C@@H](CSSC[C@@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@H]7CC8=CNC9=CC=CC=C89)=O)=O)=O)NC1=O)C(N[C@@H](CC(O)=O)C(N[C@@H](CO)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@H]2CSSC[C@@H](C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@@H](CC=CNC=CC=CC=C)C(O)=O)=O)=O)=O)=O)=O)NC7=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)[C@H](CC=CC=C(C=C)O)N–Neurological Disease–10 mM in DMSO–Sodium Channel–Nav1.7–Membrane Transporter/Ion Channel–Peptides