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TPA 023

SKU: orb1307656

Description

TPA 023 is a potent and selective agonist for GABAA receptors containing α2 and/or α3 subunits, exhibiting binding affinities in the sub-nanomolar range (Ki = 0.19 - 0.41 nM). This compound is a valuable research tool for investigating the roles of specific GABAA receptor subtypes in anxiety, sedation, and cognitive functions in both in vitro and in vivo studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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TPA 023

Key Properties

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CAS Number252977-51-8
MW395.43
Purity99.06% (May vary between batches)
FormulaC20H22FN7O
SMILESCCn1ncnc1COc1nn2c(nnc2cc1C(C)(C)C)-c1ccccc1F
TargetGABA Receptor
SolubilityDMSO:50 mg/mL (126.44 mM)

Bioactivity

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Target 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. 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.

Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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GABA Receptor, GABAA, GABAReceptor, Gamma-aminobutyric acid Receptor, Inhibitor, inhibit, TPA 023, TPA023, TPA-023, γ-Aminobutyric acid Receptor
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
9908684 ↗

Key Properties

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No computed properties available.

Protocol Information

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Available Sizes

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1 mg
$ 110.00
5 mg
$ 180.00
1 ml x 10 mM (in DMSO)
$ 190.00
10 mg
$ 240.00
25 mg
$ 380.00
50 mg
$ 590.00
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