Biological Activity
Selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Binds to closed/inactive channel. Selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Increases latency of withdrawal response in mouse tail-flick and paw-flick tests. Analgesic.
Technical Data
| M. Wt | 6554.51 |
| Formula | C272H429N85O84S10 |
| Sequence |
LKCYQHGKVVTCHRDMKFCYHNTGMPFRNLKLILQGCSSSCSETENNKCCSTDRCNK (Modifications: Disulfide bridge: 3-19, 12-37, 41-49, 50-55) |
| Storage | Store at -20°C |
| CAS Number | 1609937-15-6 |
| PubChem ID | 121513904 |
| InChI Key | JRVGGBDTNREHFW-UHFFFAOYSA-N |
| Smiles | [H]N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@H]1CSC[C@@H]2NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC3=CNC=N3)NC(=O)[C@H](CSSC[C@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC3=CC=CC=C3)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCSC)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC3=CNC=N3)NC(=O)[C@H](CC3=CC=C(O)C=C3)NC2=O)[C@@H](C)O)[C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC2=O)[C@@H](C)O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CO)NC2=O)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCN)C(O)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)CNC(=O)[C@H](CC2=CNC=N2)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC2=CC=C(O)C=C2)NC1=O)C(C)C)C(C)C)[C@@H](C)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 6554.51. 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 | 0.15 mL | 0.76 mL | 1.53 mL |
| 5 mM | 0.03 mL | 0.15 mL | 0.31 mL |
| 10 mM | 0.02 mL | 0.08 mL | 0.15 mL |
| 50 mM | 0 mL | 0.02 mL | 0.03 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Diochot et al (2012) Black mamba venom peptides target acid-sensing ion channels to abolish pain. Nature 490 552 PMID: 23034652
Keywords: Mambalgin 1, supplier, ASIC1a, inhibitors, inhibits, acid, sensing, ion, channels, analgesics, analgesia, venoms, ASIC, ASIC, Tocris Bioscience
