TCN-201|CAS 852918-02-6|DC Chemicals

Cas No.:	852918-02-6
Chemical Name:	4-[[[(3-chloro-4-fluorophenyl)sulfonyl]amino]methyl]-benzoic acid 2-benzoylhydrazide
Synonyms:	TCN-201, TCN 201, TCN201
SMILES:	O=C(NNC(C1=CC=CC=C1)=O)C2=CC=C(CNS(=O)(C3=CC=C(F)C(Cl)=C3)=O)C=C2
Formula:	C₂₁H₁₇ClFN₃O₄S
M.Wt:	461.89
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDAR. TCN 201 antagonism is dependent on the GluN1-agonist concentration. TCN 201 allows pharmacological identification of native GluN2A-containing NMDAR populations[1].
Target:	NMDAR[1]
In Vivo:	TCN-201 (10 mg/kg; i.p.) is ineffective in CSD g blood-oxygen level-dependent (BOLD) response in rats[3].
In Vitro:	TCN 201 (10 μM) produces only slight inhibition of GluN1/GluN2B NMDAR-mediated currents in oocytes[1]. TCN 201 (10-30 μM) antagonism of NMDAR-mediated responses is both subtype- and glycine-dependent and more potent than TCN 213 in oocytes[1]. TCN 201 (0.1-100 μM) does not produce complete block of NMDAR-mediated responses in oocytes[1]. TCN 201 (10 μM) antagonism of NMDAR-mediated currents shows a negative correlation with their ifenprodil sensitivity in rat cortical neurons[1]. TCN 201 (1-9 μM) suppresses cortical spreading depression (CSD) in chick retina[2].
References:	[1]. Edman S, et, al. TCN 201 selectively blocks GluN2A-containing NMDARs in a GluN1 co-agonist dependent but non-competitive manner. Neuropharmacology. 2012 Sep; 63(3): 441-9. [2]. Bu F, et, al. NR2A contributes to genesis and propagation of cortical spreading depression in rats. Sci Rep. 2016 Mar 22;6:23576. [3]. Shatillo A, et, al. Involvement of NMDA receptor subtypes in cortical spreading depression in rats assessed by fMRI. Neuropharmacology. 2015 Jun; 93:164-70.

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