TCN 201

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Cat.No. 4154 - TCN 201 | C21H17ClFN3O4S | CAS No. 852918-02-6
Description: Selective NR1/NR2A receptor antagonist
Chemical Name: 3-Chloro-4-fluoro-N-[4-[[2-(phenylcarbonyl)hydrazino]carbonyl]benzyl]benzenesulfonamide
Purity: ≥99% (HPLC)
Datasheet
Citations (7)
Literature

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.

Select a batch to recalculate based on the batch molecular weight:
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

Safety Datasheet

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


If you know of a relevant reference for TCN 201, please let us know.

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Keywords: TCN201 NMDA receptor agonist selective NR1/NR2A antagonist NMDA Receptors

7 Citations for TCN 201

Citations are publications that use Tocris products. Selected citations for TCN 201 include:

Chen et al (2016) β-arrestin-2 regulates NMDA receptor function in spinal lamina II neurons and duration of persistent pain. Nature Communications 7 12531 PMID: 27538456

Tian et al (2016) STEP activation by Gαq coupled GPCRs opposes Src regulation of NMDA receptors containing the GluN2A subunit Scientific Reports 6 36684  PMID: 27857196

Gu et al (2015) miR-26a and miR-384-5p are required for LTP maintenance and spine enlargement. Nat Commun 6 6789 PMID: 25858512

Liu et al (2015) The distinct role of NR2B subunit in the enhancement of visual plasticity in adulthood. Mol Brain 8 49 PMID: 26282667

Hu et al (2015) miR-501-3p mediates the activity-dependent regulation of the expression of AMPA receptor subunit GluA1. J Pharmacol Exp Ther 208 949 PMID: 25800054

Izumi and Zorumski (2015) Sensitivity of N-methyl-D-aspartate receptor-mediated excitatory postsynaptic potentials and synaptic plasticity to TCN 201 and TCN 213 in rat hippocampal slices. PeerJ 352 267 PMID: 25413830

Jia et al (2013) Age-dependent regulation of synaptic connections by dopamine D2 receptors. Nat Neurosci 16 1627 PMID: 24121738


Do you know of a great paper that uses TCN 201 from Tocris? If so please let us know.

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Pathways for TCN 201

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