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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Potassium Channel-GiGA1
GiGA1

Chemical Structure : GiGA1

CAS No.: 75322-58-6

GiGA1 (G-protein-independent GIRK channel activator 1)

货号: PC-23631Not For Human Use, Lab Use Only.

GiGA1 is a selective G-protein-independent activator of GIRK channels, targets the alcohol pocket and specifically activates GIRK1/GIRK2 with EC50 of 31 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

GiGA1 is a selective G-protein-independent activator of GIRK1/2 channels targets the alcohol pocket and specifically activates GIRK1/GIRK2 with EC50 of 31 uM.
GiGA1 exhibits high specificity for activating GIRK1/GIRK2 channels, GiGA1 activaiton of GIRK1/GIRK2 channels, does saturate at ~100 μM.
GiGA1 exhibits little to no activity against GIRK2/GIRK3, GIRK1/GIRK3, and GIRK1/GIRK4 channels expressed in HEK293T cells.
GiGA1 induces GIRK currents in hippocampal CA1 pyramidal neurons, which express mostly GIRK1/GIRK2 heterotetramers.
GiGA1 (20, 40, or 60 mg/ kg) exhibited antiseizure properties in an in vivo epilepsy model.

物理化学性质&存储条件

分子量 232.30
分子式 C12H12N2OS
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

1-(thiophen-2-yl)-3-(o-tolyl)urea

参考文献

1. Zhao Y, et al. Cell Rep. 2020 Jun 16;31(11):107770.

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