ProTx II
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].
Product Specifications
CAS Number
484598-36-9
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.html
Solubility
10 mM in DMSO
Smiles
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%10=CNC%11=CC=CC=C%10%11)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%12=CC=C(C=C%12)O)N
Molecular Formula
C168H250N46O41S8
Molecular Weight
3826.59
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.
Shipping Conditions
Room temperature
Scientific Category
Peptides
Clinical Information
No Development Reported
Isoform
Nav1.7
Frequently Asked Questions
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