KRM-II-81 |CAS:2014348-91-3 Probechem Biochemicals

Chemical Structure : KRM-II-81

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KRM-II-81

货号: PC-35483Not For Human Use, Lab Use Only.

KRM-II-81 is a selective α2/α3 subtype GABAA receptor ligand (positive allosteric modulator) with EC50 of 937 nM for α3β3γ2 GABAAR.

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生物&药学活性

KRM-II-81 is a selective α2/α3 subtype GABAA receptor ligand (positive allosteric modulator) with EC50 of 937 nM for α3β3γ2 GABAAR.
KRM-II-81 demonstrated similar efficacy at α1/α2/α3 GABAA receptors and negligible efficacy at α4/α5/α6 GABAA receptors, with α2 and α3-subtypes being 17- and 28-fold more potent than α1 subtypes in HEK-293T cells expressing GABAA receptors with different α subunits.
KRM-II-81 exhibited improved anxiolytic-like effects in a mouse marble burying assay and a rat Vogel conflict test.
KRM-II-81 dose-dependently decreased 0.6% acetic acid- and 0.32% lactic acid-induced writhing.
KRM-II-81 exhibited significant antinociceptive effects in chemical stimulation-induced pain in mice.

物理化学性质&存储条件

分子量	351.369
分子式	C21H13N5O
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	5-(8-ethynyl-6-(pyridin-2-yl)-4H-benzo[f]imidazo[1,5-a][1,4]diazepin-3-yl)oxazole

参考文献

1. Poe MM, et al. J Med Chem. 2016 Dec 8;59(23):10800-10806.

2. Lewter LA, et al. ACS Chem Neurosci. 2017 Jun 21;8(6):1305-1312.

KRM-II-81

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KRM-II-81

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