TCN 213 is a selective, surmountable, glycine-dependent GluN1/GluN2A NMDAR antagonist (inhibitor) with IC50s of 0.55, 3.5, and 40 μM in the presence of 75, 750, and 7500 nM glycine, respectively. TCN 213 may be utilized to pharmacologically monitor the switching of NMDAR expression in developing cortical neurons.

Physicochemical Properties

Molecular Formula	C18H24N4OS2
Molecular Weight	376.54
Exact Mass	376.139
CAS #	556803-08-8
PubChem CID	2608149
Appearance	White to off-white solid powder
LogP	4.201
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	6
Rotatable Bond Count	8
Heavy Atom Count	25
Complexity	401
Defined Atom Stereocenter Count	0
InChi Key	XBAZPYFIYYCZBO-UHFFFAOYSA-N
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)
Chemical Name	2-[[5-(benzylamino)-1,3,4-thiadiazol-2-yl]sulfanyl]-N-(cyclohexylmethyl)acetamide
HS Tariff Code	2934.99.9001
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)

Biological Activity

Targets	GluN1/GluN2A NMDAR 0.55-40 μM (IC50)
ln Vitro	NMDA-evoked currents in neurons transfected with GluN2A subunits are inhibited by TCN 213 (30 µM)[1].
References	[1]. “Direct pharmacological monitoring of the developmental switch in NMDA receptor subunit composition using TCN 213, a GluN2A-selective, glycine-dependent antagonist.” British journal of pharmacology vol. 166,3 (2012): 924-37. [2]. TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner. Neuropharmacology. 2012 Sep;63(3):441-9.

Solubility Data

Solubility (In Vitro)

DMSO: 250 mg/mL (663.94 mM)

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.