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TPA 023 is a selective agonist of GABAA α2/α3 subtype (Kis = 0.19 - 0.41 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $239 | In Stock | |
5 mg | $579 | In Stock | |
10 mg | $868 | In Stock | |
25 mg | $1,280 | In Stock | |
50 mg | $1,730 | In Stock | |
100 mg | $2,330 | In Stock | |
1 mL x 10 mM (in DMSO) | $637 | In Stock |
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 |
Smiles | CCn1ncnc1COc1nn2c(nnc2cc1C(C)(C)C)-c1ccccc1F |
Relative Density. | 1.33 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (126.44 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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