Chemical Structure : GiGA1
CAS No.:
75322-58-6
GiGA1
(G-protein-independent GIRK channel activator 1)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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232.30
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Formula
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C12H12N2OS
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(thiophen-2-yl)-3-(o-tolyl)urea
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References
1. Zhao Y, et al. Cell Rep. 2020 Jun 16;31(11):107770.
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