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TPA023B

Chemical Structure : TPA023B

CAS No.: 425377-76-0

TPA023B (TPA-023B)

Catalog No.: PC-25648Not For Human Use, Lab Use Only.

TPA023B (TPA-023B) is selective partial agonist / positive allosteric modulat of GABAA receptor α2/α3 subtype with Ki of  0.73 nM/2 nM respectively, also is an α1 subtype antagonist with Ki of 1.8 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

TPA023B (TPA-023B) is selective partial agonist / positive allosteric modulat of GABAA receptor α2/α3 subtype with Ki of  0.73 nM/2 nM respectively, also is an α1 subtype antagonist with Ki of 1.8 nM.
TPA023B has partial agonistic activity at the benzodiazepine binding site of α2β3γ2 and α3β3γ2 GABAARs, but does not potentiate α1β2γ2 GABAARs and had very weak potentiating effects on α5β2γ2 GABAARs.
TPA023B (1 mg kg−1, p.o.) exerts strong antipruritic actions in wild-type mice.
TPA023B reduces acute itch mainly through spinal α2GABAARs.
TPA023B shows antipruritic actions in a dog model of allergic itch.

Physicochemical Properties

M.Wt 391.38
Formula C21H15F2N5O
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

2',6-difluoro-5'-(3-(2-hydroxypropan-2-yl)imidazo[1,2-b][1,2,4]triazin-7-yl)-[1,1'-biphenyl]-2-carbonitrile

References

1. Atack JR, et al. J Psychopharmacol. 2011 Mar;25(3):329-44.

2. Ralvenius WT, et al. Nat Commun. 2018 Aug 13;9(1):3230.

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