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TCN-201

Cat. No. M3189
TCN-201 Structure
Size Price Availability
10mg USD 90 Out of stock
50mg USD 380 Out of stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

TCN-201 is a selective GluN2A-containing N-methyl-D-aspartate receptor (NMDAR) antagonist with IC50 of 0.326 μM. TCN-201 displays selectivity for GluN1/GluN2A NMDARs over GluN1/GluN2B containing NMDARs, in assays using two-electrode voltage-clamp (TEVC) recordings of NMDAR currents from Xenopus laevis oocytes expressing either GluN1/GluN2A or GluN1/GluN2B NMDARs. Similar to TCN 213, the degree of inhibition produced by TCN-201 is dependent on the concentration of the GluN1-site co-agonist, glycine (or D-serine), and is independent of the glutamate concentration. In regard to glycine at 3 μM, 10 μM, and 30 μM, the IC50 values of TCN-201 are 0.446 μM, 0.746 μM, and 3.89 μM, respectively, while with D-serine at 3 μM, 10 μM, and 30 μM, the IC50 values of TCN-201 are 0.326 μM, 0.816 μM, and 1.92 μM, respectively. TCN-201 acts in a non-competitive manner but its equilibrium constant at GluN1/GluN2A NMDARs indicates TCN-201 is around 30-times more potent than TCN 213. TCN-201 shows only modest antagonism of NMDAR-mediated currents recorded from young (DIV 9-10) neurones, but gives a strong block in older cultures (DIV 15-18) or in cultures where GluN2A subunits have been over-expressed. TCN-201 antagonism of NMDAR-mediated currents shows a negative correlation with their ifenprodil sensitivity and therefore, in combination with ifenprodil, can be used to monitor, pharmacologically, the expression levels of GluN2A and GluN2B NMDAR subunits in neuronal populations.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 461.89
Formula C21H17ClFN3O4S
CAS Number 852918-02-6
Purity >99%
Solubility DMSO
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: TCN-201 supplier, GluR, inhibitors

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