TDPAM02
TDPAM02 is a potent positive allosteric modulator of the AMPA receptor GluA2 subunit, with an EC50 of 1.4 nM for the GluA2 flop (Q) subunit. TDPAM02 binds at the dimer interface of the GluA2 ligand-binding domain and stabilizes the receptor conformation by simultaneously occupying two allosteric sites, thereby significantly slowing the receptor desensitization process and maintaining rapid excitatory synaptic transmission in the central nervous system. TDPAM02 is also a positive allosteric modulator of the GluK1 receptor. TDPAM02 can be used for research on neurological diseases.
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- CAS No.: 2231101-34-9
- Formule: C22H26N4O4S2
- Masse moléculaire:474.59
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
AMPA Receptor 1.4 nM (EC50, GluA2 flop (Q)) |
Kainate Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
1.4 nM
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Positive allosteric modulator potency at GluA2 flop (Q) in HEK293 cells assessed by calcium flux assay.
Positive allosteric modulator potency at GluA2 flop (Q) in HEK293 cells assessed by calcium flux assay.
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30891120 |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2231101-34-9
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Masse moléculaire 474.59
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Formule C22H26N4O4S2
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SMILES
O=S1(=O)NCN(C2=CC(=CC=C21)CCC3=CC=C4C(=C3)N(CNS4(=O)=O)C5CC5)C6CC6
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Laulumaa S, et al. Crystal Structures of Potent Dimeric Positive Allosteric Modulators at the Ligand-Binding Domain of the GluA2 Receptor. ACS medicinal chemistry letters. 2019 Mar 14;10(3):243-247. [Content Brief]
[2]. Zhigulin AS, et al. The diversity of AMPA receptor inhibition mechanisms among amidine-containing compounds. Frontiers in pharmacology. 2024;15:1467266. [Content Brief]
[3]. Bay Y, et al. Crystal structure of the GluK1 ligand-binding domain with kainate and the full-spanning positive allosteric modulator BPAM538. Journal of structural biology. 2024 Sep;216(3):108113. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TDPAM02 Related Classifications
HY-165475 Related Classifications
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