Size | Price | Stock |
---|---|---|
1mg | $450 | In-stock |
5mg | $950 | In-stock |
10mg | $1600 | In-stock |
50 mg | Get quote | |
100 mg | Get quote | |
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Cat. No. : | HY-101640 |
M.Wt: | 395.43 |
Formula: | C20H22FN7O |
Purity: | >98 % |
Solubility: | 10 mM in DMSO |
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].
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