2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. TPA-023B

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.

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TPA-023B Chemical Structure

TPA-023B Chemical Structure

CAS No. : 425377-76-0

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Based on 1 publication(s) in Google Scholar

TPA-023B Related Antibodies

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Description

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[1].

In Vitro

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 Related Antibodies
In Vivo

TPA-023B gives dose- and time-dependent occupancy of rat brain GABAA receptors as measured using an in vivo [3H]flumazenil binding assay, with 50% occupancy corresponding to a respective dose and plasma drug concentration of 0.09 mg/kg and 19 ng/mL[1].
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.
Molecular Weight

391.37

Formula

C21H15F2N5O
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

N#CC1=CC=CC(F)=C1C2=CC(C3=CN=C4N3N=CC(C(C)(O)C)=N4)=CC=C2F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5551 mL 12.7756 mL 25.5513 mL
5 mM 0.5110 mL 2.5551 mL 5.1103 mL
View the 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.

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Purity & Documentation
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
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TPA-023B Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TPA-023B425377-76-0GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorHigh-affinityα2α3α1MRK-409non-sedatinganxiolyticcurrentInhibitorinhibitorinhibit

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