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Cat. No.: HY-165475

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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.

For research use only. We do not sell to patients.

CAS No.: 2231101-34-9
Formula: C₂₂H₂₆N₄O₄S₂
Molecular Weight:474.59

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (272 KB)

TDPAM02 Chemical Structure

CAS No.: 2231101-34-9

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

IC₅₀ & Target

^[1]

AMPA Receptor

1.4 nM (EC₅₀, GluA2 flop (Q))

Kainate Receptor

All iGluR Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	EC₅₀	1.4 nM	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.	30891120

In Vitro

Glutamate Release or Receptors

TDPAM02 is a potent positive allosteric modulator of GluA2 flop (Q) in HEK293 cells, with a potency of 1.4 nM^[1].
TDPAM02 (100 µM) has a weak positive allosteric modulatory effect in GT HEK293 cells expressing GluK1 (Q) b and NETO2^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Related Protocols :

Synaptic current patch-clamp recording in brain slices

Chemical Information

CAS No. 2231101-34-9
Molecular Weight 474.59
Formula C₂₂H₂₆N₄O₄S₂
SMILES

O=S1(=O)NCN(C2=CC(=CC=C21)CCC3=CC=C4C(=C3)N(CNS4(=O)=O)C5CC5)C6CC6
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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.

[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.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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