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Chemical Structure : S44819
Catalog No.: 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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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); 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); enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy in vivo.
Stroke
Phase 2 Clinical
| M.Wt | 365.382 | |
| Formula | C19H12FN3O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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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.
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