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TPA 023

Catalog No. T17144   CAS 252977-51-8

TPA 023 is a selective agonist of GABAA α2/α3 subtype (Kis = 0.19 - 0.41 nM).

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TPA 023 Chemical Structure
TPA 023, CAS 252977-51-8
Pack Size Availability Price/USD Quantity
1 mg In stock $ 372.00
5 mg In stock $ 788.00
10 mg In stock $ 1,080.00
25 mg In stock $ 1,630.00
50 mg In stock $ 2,180.00
100 mg In stock $ 2,970.00
1 mL * 10 mM (in DMSO) In stock $ 685.00
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Purity: 99.06%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description TPA 023 is a selective agonist of GABAA α2/α3 subtype (Kis = 0.19 - 0.41 nM).
Targets&IC50 GABAA:(ki)0.19-0.41 nM
In vivo 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[1]. In rats, TPA023 (0.42 mg/kg; oral) displays good receptor occupancy and results in 50% occupancy of rat brain GABAA receptors, with the corresponding plasma concentration being 25 ng/mL. TPA023 (3 mg/kg p.o. in 0.5% methylcellulose) shows anxiolytic-like effect on rats. TPA023(10 mg/kg i.p.) is efficacious in the mouse pentylenetetrazole-induced seizure model, providing full seizure protection(84% occupancy), with the ED50 of 0.19-0.41 nM[2].
Molecular Weight 395.43
Formula C20H22FN7O
CAS No. 252977-51-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (126.44 mM)

TargetMolReferences and Literature

1. Castner SA, et al. Reversal of ketamine-induced working memory impairments by the GABAAalpha2/3 agonist TPA023. Biol Psychiatry. 2010 May 15;67(10):998-1001. 2. Atack JR. Subtype-selective GABA(A) receptor modulation yields a novel pharmacological profile: the design and development of TPA023. Adv Pharmacol. 2009;57:137-85

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Anti-Neurodegenerative Disease Compound Library Neurotransmitter Receptor Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Clinical Compound Library Bioactive Compound Library Drug Repurposing Compound Library Bioactive Compounds Library Max

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Keywords

TPA 023 252977-51-8 Membrane transporter/Ion channel Neuroscience GABA Receptor inhibit γ-Aminobutyric acid Receptor Inhibitor Gamma-aminobutyric acid Receptor TPA-023 TPA023 inhibitor

 

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