TPA023 (MK-0777) | α2/α3 GABAAR agonist | Probechem Biochemicals

Chemical Structure : TPA023

CAS No.: 252977-51-8

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TPA023 (MK-0777, MK0777, TPA-023, TPA 023)

货号: 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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10 mg	￥1480	In stock
25 mg	￥2580	In stock
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生物&药学活性

TPA023 (MK-0777) 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.
TPA023 (MK-0777) shows much lower (50- to 2000-fold) affinities for α4 and α6 subtypes (Ki= 60 and 418 nM, respectively).
TPA023 (MK-0777) demonstrates anxiolytic-like efficacy and anticonvulsant activity in mouse pentylenetetrazole seizure model.

物理化学性质&存储条件

分子量	395.442
分子式	C20H22FN7O
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	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

参考文献

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.

TPA023 (MK-0777, MK0777, TPA-023, TPA 023)

生物&药学活性

物理化学性质&存储条件

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TPA023 (MK-0777, MK0777, TPA-023, TPA 023)

生物&药学活性

物理化学性质&存储条件

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