S44819 | α5-GABAAR antagonist | Probechem Biochemicals

Chemical Structure : S44819

CAS No.: 1398496-82-6

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S44819 (S-44819, Egis-13529, Afizagabar)

货号: PC-35544Not For Human Use, Lab Use Only.

S44819 (S-44819, Egis-1352 Afizagabar) is a novel potent, competitive, selective antagonist of the α5-GABAAR with Kd of 221 nM, IC50 of 585 nM (α5β2γ2).

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生物&药学活性

S44819 (S-44819, Egis-1352 Afizagabar) is a novel potent, competitive, selective antagonist of the α5-GABAAR with Kd of 221 nM, IC50 of 585 nM (α5β2γ2).
S44819 does not inhibit the activation of α5-GABAARs by etomidate, displays week activity against α1β2γ2 (IC50=2.4 uM) and α3β2γ2 (IC50=3.7 uM).
S44819 enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy in vivo.

物理化学性质&存储条件

分子量	365.382
分子式	C19H12FN3O2S
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-(4-Fluoro-1-benzothiophen-2-yl)-8-methyl-1,9-dihydro2H-[1,3]oxazolo[4,5-H][2,3]benzodiazepin-2-one

参考文献

1. Darmani G, et al. J Neurosci. 2016 Dec 7;36(49):12312-12320.

2. Gacsályi I, et al. Neuropharmacology. 2017 Oct;125:30-38.

3. Etherington LA, et al. Neuropharmacology. 2017 Oct;125:353-364.

4. Gacsályi I, et al. Eur J Pharmacol. 2018 Jul 21;834:118-125.

S44819 (S-44819, Egis-13529, Afizagabar)

生物&药学活性

物理化学性质&存储条件

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S44819 (S-44819, Egis-13529, Afizagabar)

生物&药学活性

物理化学性质&存储条件

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