Biological Activity
Potent and selective acid-sensing ion channel 1a (ASIC1a) blocker (IC50 = 0.9 nM). Displays no effect at ASIC1b, ASIC2a, ASIC3, heteromeric ASIC channels, ENaC and KV2.1/2.2/4.2/4.3 channels expressed in oocytes, at concentrations up to 100 nM. Displays potent analgesic properties against thermal, mechanical, chemical, inflammatory and neuropathic pain in rodents.
Technical Data
| M. Wt | 4689.41 |
| Formula | C200H312N62O57S6 |
| Sequence |
EDCIPKWKGCVNRHGDCCEGLECWKRRRSFEVCVPKTPKT (Modifications: Disulfide bridge: 3-18, 10-23, 17-33) |
| Storage | Store at -20°C |
| PubChem ID | 90489000 |
| InChI Key | LICLJUGDURFZIM-UHFFFAOYSA-N |
| Smiles | [H]N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CO)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CSSC[C@H](NC(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]4CCCN4C(=O)[C@@H](NC1=O)[C@@H](C)CC)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC1=CNC=N1)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(=O)N3)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC2=O)C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)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 2 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 4689.41. 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 | 0.21 mL | 1.07 mL | 2.13 mL |
| 5 mM | 0.04 mL | 0.21 mL | 0.43 mL |
| 10 mM | 0.02 mL | 0.11 mL | 0.21 mL |
| 50 mM | 0 mL | 0.02 mL | 0.04 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Mazzuca et al (2007) A tarantula peptide against pain via ASIC1a channels and opioid mechanisms. Nat.Neurosci. 10 943 PMID: 17632507
Escoubas et al (2000) Isolation of a tarantula toxin specific for a class of proton-gated Na+ channels. J.Biol.Chem. 275 25116 PMID: 10829030
Escoubas et al (2003) Recombinant production and solution structure of PcTx1, the specific peptide inhibitor of ASIC1a proton-gated cation channels. Protein Sci. 12 1332 PMID: 12824480
Salinas et al (2006) The receptor site of the spider toxin PcTx1 on the proton-gated cation channel ASIC1a. J.Physiol. 570 339 PMID: 16284080
Keywords: Psalmotoxin 1, supplier, pctx1, acid-sensing, acid, ion, channel, 1a, ASIC1a, ASIC, blockers, analgesic, pain, thermal, mechanical, chemical, inflammatory, neuropathic, venoms, PcTx1, ASIC, ASIC, Tocris Bioscience
