ProTx II (TFA)

ProTx II TFA 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].

Product Specifications

UNSPSC

12352209

Target

Sodium Channel

Type

Peptides

Related Pathways

Membrane Transporter/Ion Channel

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/protx-ii-tfa.html

Purity

99.72

Solubility

DMSO : 50 mg/mL (ultrasonic) |H2O : 100 mg/mL (ultrasonic)

Smiles

O=C([C@@H](N)CC1=CC=C(O)C=C1)N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H]2CSSC[C@H](NC3=O)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(O)=O)CC4=CNC5=CC=CC=C45)=O)CC(C)C)=O)CCCCN)=O)CCCCN)=O)CCCCN)=O)=O)CCCCN)=O)CCCNC(N)=N)=O)CCC(O)=O)=O)CO)=O)CC(O)=O)=O)CSSC[C@H](NC6=O)C(N[C@H](C(N[C@H](C(N[C@H]3CC7=CNC8=CC=CC=C78)=O)CC(C)C)=O)CCCNC(N)=N)=O)=O)[C@@H](C)O)=O)CC9=CNC%10=CC=CC=C9%10)=O)CCSC)=O)CC%11=CNC%12=CC=CC=C%11%12)=O)CCCCN)=O)CCC(N)=O)=O)CSSC[C@H](NC2=O)C(N[C@H](C(NCC(N[C@H](C(N[C@H]6C(C)C)=O)CCSC)=O)=O)CCC(O)=O)=O.CC(C(F)(F)F)=O.[x]

Molecular Formula

C168H250N46O41S8.xC2HF3O2

Molecular Weight

3826.59 (free base)

References & Citations

[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.