1781880-44-1
1781880-44-1 structure
- Name: PHP 501 trifluoroacetate
- Chemical Name: GABAA receptor agent 2 TFA
- CAS Number: 1781880-44-1
- Molecular Formula: C22H22F3N3O3
- Molecular Weight: 433.42
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel GABA Receptor
- Create Date: 2020-08-07 15:54:57
- Modify Date: 2024-01-12 19:58:17
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GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3)[1].
| Name | GABAA receptor agent 2 TFA |
|---|
| Description | GABAA receptor agent 2 TFA is a potent and high-affinity GABAA receptor antagonist with an IC50 of 24 nM (human α1β2γ2 GABAA-expressing tsA201 cells) and a Ki of 28 nM (rat GABAA receptors). GABAA receptor agent 2 TFA is inactive against four human GABA transporters (hGAT-1, hBGT-1, hGAT-2, and hGAT-3)[1]. |
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| Related Catalog | |
| Target |
IC50: 24 nM (Human α1β2γ2 GABAA-expressing tsA201 cells)[1] Ki: 28 nM (Rat GABAA receptors)[1] |
| In Vitro | With the protonated piperidine nitrogen consistently placed to interact with β2 E155, only a simultaneous interaction with α1 R66 provided enough space above and below the ligand heteroaromatic ring to be compatible with the high affinity (0.022 μM) of the disubstituted GABAA receptor agent 2 (compound 19)[2]. |
| References |
| Molecular Formula | C22H22F3N3O3 |
|---|---|
| Molecular Weight | 433.42 |