Biological Activity
Kv2.1 and Kv2.2 channel blocker (IC50 values are 1-3 nM). Enhances glucose-stimulated insulin secretion from human islets in vitro, but not from islet cells lacking the Kv2.1 channel. Has no significant effect on plasma insulin, glucagon or blood glucose levels in mice, but increases plasma somatostatin levels.
Technical Data
| M. Wt | 3948.61 |
| Formula | C178H248N44O45S7 |
| Sequence |
EGECGGFWWKCGSGKPACCPKYVCSPKWGLCNFPMP (Modifications: Disulfide bridge: 4-19,11-24,18-31) |
| Storage | Store at -20°C |
| CAS Number | 1233152-82-3 |
| PubChem ID | 121513878 |
| InChI Key | SZVUKNYCMKWHNH-UHFFFAOYSA-N |
| Smiles | [H]N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H]3CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)CNC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]4CCCN4C(=O)[C@H](CO)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC4=CNC5=C4C=CC=C5)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)CNC(=O)CNC1=O)C(=O)NCC(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N3)NC(=O)[C@@H](NC(=O)[C@H](CC1=CC=C(O)C=C1)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C2=O)C(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCSC)C(=O)N1CCC[C@H]1C(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 3948.61. 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 | 0.25 mL | 1.27 mL | 2.53 mL |
| 5 mM | 0.05 mL | 0.25 mL | 0.51 mL |
| 10 mM | 0.03 mL | 0.13 mL | 0.25 mL |
| 50 mM | 0.01 mL | 0.03 mL | 0.05 mL |
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References
References are publications that support the products' biological activity.
Li et al (2013) The role of voltage-gated potassium channels Kv2.1 and Kv2.2 in the regulation of insulin and somatostatin release from pancreatic islets. J.Pharmacol.Exp.Ther. 344 407 PMID: 23161216
Herrington (2007) Gating modifier peptides as probes of pancreatic beta-cell physiology. Toxicon 49 231 PMID: 17101164
Keywords: Guangxitoxin 1E, supplier, Kv2.1, Kv2.2, inward, rectifier, potassium, current, pancreatic, islets, beta, cells, inhibits, inhibitors, insulin, glucose, somatostatin, GxTx-1E, venoms, Voltage-Gated, Potassium, Channels, Voltage-Gated, Potassium, Channels, Tocris Bioscience
