Product overview
| Name | TCN 201 |
| Description | Potent, non-competitive GluN2A subunit selective NMDA receptor antagonist |
| Purity | >99% |
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Biological Data
| Biological description | Potent and non-competitive GluN2A subunit selective NMDA receptor antagonist (pIC50 values are 6.8 and <4.3 for GluN2A and GluN2B respectively in a FLIPR/Ca2+ assay). Binds at allosteric site. Inhibition is GluN1 co-agonist (glycine or D-serine) concentration dependent. Shows anti-nicotine addiction effects. |
Solubility & Handling
| Storage instructions | +4°C |
| Solubility overview | Soluble in DMSO (100mM) |
| Important | This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use. |
Chemical Data
| Chemical name | 3-Chloro-4-fluoro-N-[4-[[2-(phenylcarbonyl)hydrazino]carbonyl]benzyl]benzenesulfonamide |
| Molecular Weight | 461.89 |
| Chemical structure |  |
| Molecular Formula | C21H17ClFN3O4S |
| CAS Number | 852918-02-6 |
| PubChem identifier | 4787937 |
| SMILES | C1=CC=C(C=C1)C(=O)NNC(=O)C2=CC=C(C=C2)CNS(=O)(=O)C3=CC(=C(C=C3)F)Cl |
| InChi | InChI=1S/C21H17ClFN3O4S/c22-18-12-17(10-11-19(18)23)31(29,30)24-13-14-6-8-16(9-7-14)21(28)26-25-20(27)15-4-2-1-3-5-15/h1-12,24H,13H2,(H,25,27)(H,26,28) |
| InChiKey | FYIBXBFDXNPBSF-UHFFFAOYSA-N |
| MDL number | MFCD06683895 |
| Appearance | White solid |
References for TCN 201
References are publications that support the biological activity of the product
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Reinstatement of nicotine seeking is mediated by glutamatergic plasticity.
Gipson CD et al (2013) Proc Natl Acad Sci U S A 110(22) : 9124-9. -
Subunit-selective allosteric inhibition of glycine binding to NMDA receptors.
Hansen KB et al (2012) J Neurosci 32(18) : 6197-208. -
TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner.
Edman S et al (2012) Neuropharmacology 63(3) : 441-9. -
Identification and characterization of novel NMDA receptor antagonists selective for NR2A- over NR2B-containing receptors.
Bettini E et al (2010) J Pharmacol Exp Ther 335(3) : 636-44.
Publications
These publications cite the use of TCN 201 purchased from Hello Bio:
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The NMDA receptor intracellular C-terminal domains reciprocally interact with allosteric modulators.
Sapkota et al (2019) Biochem Pharmacol 159 : 140-153PubMedID: 30503374 -
Structural Basis for Negative Allosteric Modulation of GluN2A-Containing NMDA Receptors.
Yi et al (2016) Neuron 91(6) : 1316-29PubMedID: 27618671
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