Biological Activity
NMDA receptor antagonist selective for NR1/NR2A over NR1/NR2B-containing receptors (pIC50 values are 6.8 and <4.3, respectively, in human recombinant NR1/NR2A and NR1/NR2B FLIPR/Ca2+ assays).
Compound Libraries
TCN 201 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 461.89 |
| Formula | C21H17ClFN3O4S |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 852918-02-6 |
| PubChem ID | 4787937 |
| InChI Key | FYIBXBFDXNPBSF-UHFFFAOYSA-N |
| Smiles | ClC1=C(F)C=CC(S(NCC2=CC=C(C(NNC(C3=CC=CC=C3)=O)=O)C=C2)(=O)=O)=C1 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.19 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 461.89. 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 | 2.17 mL | 10.83 mL | 21.65 mL |
| 5 mM | 0.43 mL | 2.17 mL | 4.33 mL |
| 10 mM | 0.22 mL | 1.08 mL | 2.17 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.43 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bettini et al (2010) Identification and characterization of novel NMDA receptor antagonists selective for NR2A- over NR2B-containing receptors. J.Pharm.Exp.Ther. 335 644 PMID: 20810618
Shin et al (2011) Subtype selective NMDA receptor antagonists induce recovery of synapses lost following exposure to HIV-1 Tat. Br.J.Pharmacol. 166 1002 PMID: 22142193
Edman et al (2012) TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner. Neuropharmacology 63 441 PMID: 22579927
Hansen et al (2012) Subunit-selective allosteric inhibition of glycine binding to NMDA receptors. J.Neurosci. 32 6197 PMID: 22553026
Gipson et al (2013) Reinstatement of nicotine seeking is mediated by glutamatergic plasticity. Proc.Natl.Acad.Sci.U S A [Epub ahead of print] PMID: 23671067
Keywords: TCN 201, supplier, TCN201, NMDA, receptor, agonist, selective, NR1/NR2A, antagonist, NMDA, Receptors, NMDA, Receptors, Tocris Bioscience
