TPA023B (TPA-023B)

Chemical Structure : TPA023B

CAS No.: 425377-76-0

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货号: 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.

规格	价格	库存
2 mg	￥1880	In stock
5 mg	￥2980	In stock
10 mg	￥4880	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	391.38
分子式	C21H15F2N5O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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.

TPA023B (TPA-023B)

生物&药学活性

物理化学性质&存储条件

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TPA023B (TPA-023B)

生物&药学活性

物理化学性质&存储条件

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