Biological Activity
NR2B-selective, competitive antagonist of the NMDA receptor. Blocks NMDA-evoked current in mouse cortical neurons (IC50 = 480 nM); also inhibits NMDA-evoked responses in oocytes expressing N2RB, but not NR2A, subunits (IC50 ~300 nM). Exhibits neuroprotective properties in vivo and in vitro.
Technical Data
M. Wt | 2264.21 |
Formula | C88H138N26O44 |
Sequence |
GEXXLQXNQXLIRXKSN (Modifications: X = Gla, Asn-17 = C-terminal amide) |
Storage | Store at -20°C |
CAS Number | 93438-65-4 |
PubChem ID | 16132376 |
InChI Key | HTBKFGWATIYCSF-UHFFFAOYSA-N |
Smiles | CCC(C)C(NC(=O)C(CC(C)C)NC(=O)C(CC(C(O)=O)C(O)=O)NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(CC(C(O)=O)C(O)=O)NC(=O)C(CCC(N)=O)NC(=O)C(CC(C)C)NC(=O)C(CC(C(O)=O)C(O)=O)NC(=O)C(CC(C(O)=O)C(O)=O)NC(=O)C(CCC(O)=O)NC(=O)CN)C(=O)NC(CCCNC(N)=N)C(=O)NC(CC(C(O)=O)C(O)=O)C(=O)NC(CCCCN)C(=O)NC(CO)C(=O)NC(CC(N)=O)C(N)=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 2264.21. 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 | 0.44 mL | 2.21 mL | 4.42 mL |
5 mM | 0.09 mL | 0.44 mL | 0.88 mL |
10 mM | 0.04 mL | 0.22 mL | 0.44 mL |
50 mM | 0.01 mL | 0.04 mL | 0.09 mL |
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References
References are publications that support the products' biological activity.
Donevan and McCabe (2000) Conantokin G is an NR2B-selective competitive antagonist of N-methyl-D-aspartate receptors. Mol.Pharmacol. 58 614 PMID: 10953056
Bush et al (2000) Selective antagonism of nigral neuropeptide responses to methamphetamine by conantokin G, a naturally occurring conopeptide. Eur.J.Pharmacol. 387 55 PMID: 10633160
Williams et al (2000) Neuroprotective efficacy and therapeutic window of the high-affinity N-methyl-D-aspartate antagonist conantokin-G: in vitro (primary cerebellar neurons) and in vivo (rat model of transient focal brain ischemia) studies. J.Pharmacol.Exp.Ther. 294 378 PMID: 10871336
Keywords: Conantokin G, supplier, neuroprotective, NMDA, receptors, antagonists, NR2B, selective, venoms, NMDA, Receptors, Tocris Bioscience