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

TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.

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

TPA 023 Chemical Structure

TPA 023 Chemical Structure

CAS No. : 252977-51-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 770 In-stock
Solution
10 mM * 1 mL in DMSO USD 770 In-stock
Solid
1 mg USD 290 In-stock
5 mg USD 700 In-stock
10 mg USD 1050 In-stock
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Based on 1 publication(s) in Google Scholar

TPA 023 Related Antibodies

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Description

TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.

IC50 & Target

Ki: 0.19-0.41 nM (GABAA)[1]
In Vivo

TPA023 displays good receptor occupancy, when administered orally to rats. The dose of TPA023 resulting in 50% occupancy of rat brain GABAA receptors is 0.42 mg/kg, with the corresponding plasma concentration being 25 ng/mL. TPA023 is also efficacious in the mouse pentylenetetrazole-induced seizure model, providing full seizure protection at a dose of 10 mg/kg i.p. (84% occupancy), with the ED50 of 0.19-0.41 nM, for protection against tonic convulsions (1.4 mg/kg i.p.) corresponding to around 50% occupancy. TPA023 (3 mg/kg p.o. in 0.5% methyl cellulose) shows anxiolytic-like effect on rats[1]. TPA023 (0.7, 2.0, and 5 mg/kg, p.o.) blocks ketamine's cognitive-impairing ability but does not influence the behavioral symptoms of rhesus monkeys[2].

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

395.43

Formula

C20H22FN7O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=CC=CC=C1C2=NN=C3C=C(C(C)(C)C)C(OCC4=NC=NN4CC)=NN32
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 : 50 mg/mL (126.44 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 2.5289 mL 12.6445 mL 25.2889 mL
5 mM 0.5058 mL 2.5289 mL 5.0578 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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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.76%

COA (255 KB) LCMS (92 KB)

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 2.5289 mL 12.6445 mL 25.2889 mL 63.2223 mL
5 mM 0.5058 mL 2.5289 mL 5.0578 mL 12.6445 mL
10 mM 0.2529 mL 1.2644 mL 2.5289 mL 6.3222 mL
15 mM 0.1686 mL 0.8430 mL 1.6859 mL 4.2148 mL
20 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1611 mL
25 mM 0.1012 mL 0.5058 mL 1.0116 mL 2.5289 mL
30 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1074 mL
40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5806 mL
50 mM 0.0506 mL 0.2529 mL 0.5058 mL 1.2644 mL
60 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0537 mL
80 mM 0.0316 mL 0.1581 mL 0.3161 mL 0.7903 mL
100 mM 0.0253 mL 0.1264 mL 0.2529 mL 0.6322 mL
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TPA 023 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 023252977-51-8TPA023TPA-023GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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