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- Afizagabar
Afizagabar
Afizagabar (S44819) 是一种首创的，有竞争性的，选择性的 α5-GABAAR 拮抗剂，对α5β2γ2 的IC50 值 585 nM，对 α5β3γ2 的 Ki 为 66 nM。Afizagabar 增强海马突触可塑性并显示促认知功效。
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包装价格促销价数量
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5mg￥5400.004320.00- +
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10mg￥9175.007340.00- +
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25mg￥19237.0015390.00- +
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50mg￥32062.0025650.00- +
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100mg￥49162.0039330.00- +
- 货号: ajcx34492
- CAS: 1398496-82-6
- 别名: S44819; Egis-13529
- 分子式: C19H12FN3O2S
- 分子量: 365.38
- 纯度: ＞98%
- 溶解度: DMSO : 6.25 mg/mL (17.11 mM; Need ultrasonic)
- 储存: Store at -20°C
- 库存: 现货
Background
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy[1].
Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons[1].
Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine[1].
[1]. Etherington LA, et al. Selective inhibition of extra-synaptic α5-GABAA receptors by S44819, a new therapeutic agent. Neuropharmacology. 2017;125:353-364.
