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TPA023

Chemical Structure : TPA023

CAS No.: 252977-51-8

TPA023 ( MK-0777)

Catalog No.: PC-62769Not For Human Use, Lab Use Only.

TPA023 is a potent, α2/α3 subtype-selective, and oral GABAA receptor agonist with Kd of 0.92, 1.05 and 0.58 nM for α1-, α2-, α3-, and α5-containing human receptors.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

TPA023 is a potent, α2/α3 subtype-selective, and oral GABAA receptor agonist with Kd of 0.92, 1.05 and 0.58 nM for α1-, α2-, α3-, and α5-containing human receptors; shows much lower (50- to 2000-fold) affinities for α4 and α6 subtypes (Ki= 60 and 418 nM, respectively); demonstrates anxiolytic-like efficacy and anticonvulsant activity in mouse pentylenetetrazole seizure model.

Anxiety

Discontinued

Physicochemical Properties

M.Wt 395.442
Formula C20H22FN7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

7-(1,1-Dimethylethyl)-6-(2-ethyl-2H-1,2,4-triazol-3-ylmethoxy)-3-(2-fluorophenyl)-1,2,4-triazolo[4,3-b]pyridazine

References

1. Atack JR, et al. J Pharmacol Exp Ther. 2010 Jan;332(1):17-25.

2. de Haas SL, et al. J Psychopharmacol. 2007 Jun;21(4):374-83.

3. Carling RW, et al. J Med Chem. 2005 Nov 17;48(23):7089-92.

4. Atack JR, et al. J Pharmacol Exp Ther. 2006 Jan;316(1):410-22.

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