| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
GluN1/GluN2A NMDAR 0.55-40 μM (IC50)
GluN1/GluN2A (NR1/NR2A) NMDA receptor. TCN 213 is a selective antagonist at the glycine modulatory site of GluN2A-containing NMDA receptors. |
|---|---|
| ln Vitro |
NMDA-evoked currents in neurons transfected with GluN2A subunits are inhibited by TCN 213 (30 µM)[1].
TCN 213 is a selective, surmountable, glycine-dependent GluN1/GluN2A NMDAR antagonist. It exhibits IC50 values of 0.55 μM, 3.5 μM, and 40 μM in the presence of 75, 750, and 7500 nM glycine, respectively. The compound shows selectivity for GluN1/GluN2A (pIC50 = 5.4) over GluN1/GluN2B-containing receptors. As a glycine-dependent antagonist, its potency decreases as glycine concentration increases, which is characteristic of glycine site antagonists. |
| ln Vivo |
No detailed in vivo activity data are publicly available for TCN 213. As a selective GluN2A antagonist, its in vivo effects would be expected to be related to modulation of GluN2A-containing NMDA receptor-mediated synaptic transmission. GluN2A-containing NMDA receptors are involved in various physiological processes, including synaptic plasticity, learning, and memory. The compound could be used in animal models to study the role of GluN2A in neurological disorders.
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| Enzyme Assay |
In vitro receptor binding assays for TCN 213 are performed to evaluate its affinity for the NMDA receptor glycine site. Radioligand binding studies using membrane preparations from cells expressing GluN1/GluN2A or GluN1/GluN2B receptors are conducted. The compound's ability to displace a specific radiolabeled glycine site ligand is measured to calculate its binding affinity. The selectivity of TCN 213 for GluN2A over GluN2B is confirmed by comparing its activity at both receptor subtypes.
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| Cell Assay |
In vitro cell-based assays are conducted using cells expressing recombinant GluN1/GluN2A or GluN1/GluN2B NMDA receptors. The cells are treated with TCN 213 in the presence of varying concentrations of glycine, and receptor activity is measured by assessing downstream signaling events such as calcium mobilization or electrophysiological responses. The glycine-dependent nature of the antagonism is characterized by determining the IC50 at different glycine concentrations.
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| Animal Protocol |
In vivo studies would be conducted in animal models to evaluate the effects of TCN 213 on NMDA receptor-mediated processes. The compound could be administered via various routes, and its effects on synaptic plasticity, learning, memory, and neurological disorders could be assessed. However, no specific in vivo data are publicly available for this compound.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data are publicly available for TCN 213. As a research compound, its ADME properties would be characterized in standard preclinical studies to guide in vivo experiments. The compound's ability to cross the blood-brain barrier is a key parameter for its use in CNS research.
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| Toxicity/Toxicokinetics |
No specific toxicity data are publicly available for TCN 213. As an NMDA receptor antagonist, its toxicity profile would be expected to be related to its mechanism of action. Excessive NMDA receptor inhibition can impair synaptic plasticity and cognitive function.
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| References |
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| Additional Infomation |
TCN 213 is a selective, surmountable, glycine-dependent GluN1/GluN2A NMDAR antagonist used as a pharmacological tool to study the role of GluN2A-containing NMDA receptors in various physiological and pathological processes. It can be used to pharmacologically monitor the switch in NMDAR expression in developing cortical neurons. The compound is not approved for human therapeutic use and is strictly for research purposes.
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| Molecular Formula |
C18H24N4OS2
|
|---|---|
| Molecular Weight |
376.54
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| Exact Mass |
376.139
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| CAS # |
556803-08-8
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| PubChem CID |
2608149
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| Appearance |
White to off-white solid powder
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| LogP |
4.201
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
25
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| Complexity |
401
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1CCC(CC1)CNC(=O)CSC2=NN=C(S2)NCC3=CC=CC=C3
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| InChi Key |
XBAZPYFIYYCZBO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H24N4OS2/c23-16(19-11-14-7-3-1-4-8-14)13-24-18-22-21-17(25-18)20-12-15-9-5-2-6-10-15/h2,5-6,9-10,14H,1,3-4,7-8,11-13H2,(H,19,23)(H,20,21)
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| Chemical Name |
2-[[5-(benzylamino)-1,3,4-thiadiazol-2-yl]sulfanyl]-N-(cyclohexylmethyl)acetamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 250 mg/mL (663.94 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6558 mL | 13.2788 mL | 26.5576 mL | |
| 5 mM | 0.5312 mL | 2.6558 mL | 5.3115 mL | |
| 10 mM | 0.2656 mL | 1.3279 mL | 2.6558 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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