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 番号: 2231101-34-9
- 分子式: C22H26N4O4S2
- 分子量:474.59
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
iGluR アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
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 |
体外実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 2231101-34-9
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分子量 474.59
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
TDPAM02 関連分類
HY-165475 関連分類
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