TPA-023B
Based on 1 Customer Validation
TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.
For research use only. We do not sell to patients.
- Purity: 98.45%
- CAS No.: 425377-76-0
- Formula: C21H15F2N5O
- Molecular Weight:391.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
TPA-023B also has high affinity for α5 subtype (Ki of 1.1 nM) of human recombinant GABAA receptor, but over 1500-fold lower for the α4- and α6 containing subtypes (Ki > 1000 nM). TPA-023B also has a comparable affinity for native rat GABAA receptors in different regions of the CNS (Ki of 0.32-0.99 nM in cerebellum, spinal cord and frontal cortex)[1].
TPA-023B antagonizes the ability of chlordiazepoxide to potentiate the GABA EC20-induced current in cells expressing the α1 subtype. More specifically, 3 μM chlordiazepoxide potentiates the GABA EC20 current by 105% and this effect could be reduced to 8% in the presence of 100 nM TPA-023B[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TPA-023B is anxiolytic in rodent and primate (squirrel monkey) models of anxiety (elevated plus maze, fear-potentiated startle, conditioned suppression of drinking, conditioned emotional response) yet has no significant effects in rodent or primate assays of ataxia and/or myorelaxation (rotarod, chain-pulling, lever pressing), up to doses (10 mg/kg) corresponding to occupancy of greater than 99%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 425377-76-0
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Appearance Solid
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Molecular Weight 391.37
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Formula C21H15F2N5O
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Color Light yellow to green yellow
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SMILES
N#CC1=CC=CC(F)=C1C2=CC(C3=CN=C4N3N=CC(C(C)(O)C)=N4)=CC=C2F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (255.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5551 mL | 12.7756 mL | 25.5513 mL | 63.8782 mL |
| 5 mM | 0.5110 mL | 2.5551 mL | 5.1103 mL | 12.7756 mL | |
| 10 mM | 0.2555 mL | 1.2776 mL | 2.5551 mL | 6.3878 mL | |
| 15 mM | 0.1703 mL | 0.8517 mL | 1.7034 mL | 4.2585 mL | |
| 20 mM | 0.1278 mL | 0.6388 mL | 1.2776 mL | 3.1939 mL | |
| 25 mM | 0.1022 mL | 0.5110 mL | 1.0221 mL | 2.5551 mL | |
| 30 mM | 0.0852 mL | 0.4259 mL | 0.8517 mL | 2.1293 mL | |
| 40 mM | 0.0639 mL | 0.3194 mL | 0.6388 mL | 1.5970 mL | |
| 50 mM | 0.0511 mL | 0.2555 mL | 0.5110 mL | 1.2776 mL | |
| 60 mM | 0.0426 mL | 0.2129 mL | 0.4259 mL | 1.0646 mL | |
| 80 mM | 0.0319 mL | 0.1597 mL | 0.3194 mL | 0.7985 mL | |
| 100 mM | 0.0256 mL | 0.1278 mL | 0.2555 mL | 0.6388 mL |
TPA-023B Related Classifications
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