Biological Activity
Selective NaV1.7 channel blocker. Shifts activation gating positively and decreases current magnitude. Displays 100-fold selectivity over other sodium channel subtypes.
Technical Data
| M. Wt | 3826.59 |
| Formula | C168H250N46O41S8 |
| Sequence |
YCQKWMWTCDSERKCCEGMVCRLWCKKKLW (Modifications: Disulfide bridge: 2-16, 9-21, 15-25) |
| Storage | Store at -20°C |
| CAS Number | 484598-36-9 |
| PubChem ID | 118708662 |
| InChI Key | XOAUGYVLRSCGBG-ZJDFQAAZSA-N |
| Smiles | [H]N[C@@H](CC1=CC=C(O)C=C1)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCC(N)=O)NC1=O)[C@@H](C)O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N3)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC2=O)C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1=CNC2=C1C=CC=C2)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 1 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 3826.59. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.26 mL | 1.31 mL | 2.61 mL |
| 5 mM | 0.05 mL | 0.26 mL | 0.52 mL |
| 10 mM | 0.03 mL | 0.13 mL | 0.26 mL |
| 50 mM | 0.01 mL | 0.03 mL | 0.05 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Smith et al (2007) Molecular interactions of the gating modifier toxin ProTx-II with NaV 1.5: implied existence of a novel toxin binding site coupled to activation. J.Biol.Chem. 282 12687 PMID: 17339321
Edgerton et al (2008) Evidence for multiple effects of ProTxII on activation gating in NaV 1.5. Toxicon. 52 489 PMID: 18657562
Schmalhofer et al (2008) ProTx-II, a selective inhibitor of NaV 1.7 sodium channels, blocks action potential propagation in nociceptors. Mol.Pharmacol. 74 1476 PMID: 18728100
Keywords: ProTx II, supplier, toxins, voltage, gated, sodium, Na+, channels, NaV1.7, potent, selective, blockers, venoms, Voltage-gated, Sodium, Channels, Voltage-gated, Sodium, Channels, Tocris Bioscience
