TPMPA
Based on 1 publication(s) in Google Scholar
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). TPMPA has the potential for the research of suppressing orientation selectivity in ganglion cells.
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- Pureza: 99.9%
- No. CAS: 182485-36-5
- Fòrmula: C6H12NO2P
- Peso molecular:161.14
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Almacenamiento:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) TPMPA
More
Actividad biológica
KB: 2.1 μM (GABAC)
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Oocyte | EC50 |
500 μM
Compound: 3, TPMPA
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Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
Agonist activity at human GABAb 1A/2 receptor expressed in Xenopus oocytes assessed as whole cell current production by two electrode voltage clamp method
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[PMID: 18528996] |
| Oocyte | EC50 |
500 μM
Compound: 3, TPMPA
|
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAb 1b/2 receptor expressed in Xenopus laevis oocytes co-expressing GIRK1/4 assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
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[PMID: 24900248] |
| Oocyte | IC50 |
0.67 μM
Compound: TPMPA
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Antagonist activity at GABAC rho1 receptor expressed in Xenopus laevis oocytes assessed as reduction of GABA-induced chloride ion currents
Antagonist activity at GABAC rho1 receptor expressed in Xenopus laevis oocytes assessed as reduction of GABA-induced chloride ion currents
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[PMID: 17467985] |
| Oocyte | IC50 |
2.22 μM
Compound: 3, TPMPA
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Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAc rho-1 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
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[PMID: 24900248] |
| Oocyte | IC50 |
22.09 μM
Compound: 3, TPMPA
|
Antagonist activity at human recombinant GABAc rho-2 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
Antagonist activity at human recombinant GABAc rho-2 receptor expressed in Xenopus laevis oocytes assessed as inhibition of GABA-induced current by two electrode voltage clamp technique
|
[PMID: 24900248] |
TPMPA antagonizes the GABA currents of ρ1 receptors (IC50 = 1.6 μM) and those of the chimeric ρ1/α1 receptors with approximately the same potency (IC50 = 1.3 μM)[1].
TPMPA shows weak activity against rho-1 and rho-2 receptors, with the KB values of 2.0 and 15.6 μM, respectively[2]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 182485-36-5
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Appearance Solid
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Peso molecular 161.14
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Fòrmula C6H12NO2P
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Color White to off-white
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SMILES
O=P(C1=CCNCC1)(C)O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
H2O : 25 mg/mL (155.14 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Martínez-Torres A, et al. GABArho 1/GABAAalpha 1 receptor chimeras to study receptor desensitization. Proc Natl Acad Sci U S A. 2000;97(7):3562-3566. [Content Brief]
[2]. Graham A. R. Johnston, et al. Neurologically-active compounds. WO1998058939A1
[3]. Johnston GA. GABAc receptors: relatively simple transmitter -gated ion channels?. Trends Pharmacol Sci. 1996;17(9):319-323. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 6.2058 mL | 31.0289 mL | 62.0578 mL | 155.1446 mL |
| 5 mM | 1.2412 mL | 6.2058 mL | 12.4116 mL | 31.0289 mL | |
| 10 mM | 0.6206 mL | 3.1029 mL | 6.2058 mL | 15.5145 mL | |
| 15 mM | 0.4137 mL | 2.0686 mL | 4.1372 mL | 10.3430 mL | |
| 20 mM | 0.3103 mL | 1.5514 mL | 3.1029 mL | 7.7572 mL | |
| 25 mM | 0.2482 mL | 1.2412 mL | 2.4823 mL | 6.2058 mL | |
| 30 mM | 0.2069 mL | 1.0343 mL | 2.0686 mL | 5.1715 mL | |
| 40 mM | 0.1551 mL | 0.7757 mL | 1.5514 mL | 3.8786 mL | |
| 50 mM | 0.1241 mL | 0.6206 mL | 1.2412 mL | 3.1029 mL | |
| 60 mM | 0.1034 mL | 0.5171 mL | 1.0343 mL | 2.5857 mL | |
| 80 mM | 0.0776 mL | 0.3879 mL | 0.7757 mL | 1.9393 mL | |
| 100 mM | 0.0621 mL | 0.3103 mL | 0.6206 mL | 1.5514 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
TPMPA Related Classifications
HY-101359 Related Classifications
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