Afizagabar S44819; Egis-13529,98.23%

产品编号:Bellancom-120051| CAS NO:1398496-82-6| 分子式:C19H12FN3O2S| 分子量:365.38

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货号 包装 价格 库存与货期 购买量 操作
Bellancom-120051
5000.00 杭州 北京(现货)
Bellancom-120051
8500.00 杭州 北京(现货)
Bellancom-120051
18000.00 杭州 北京(现货)
Bellancom-120051
30000.00 杭州 北京(现货)
Bellancom-120051
46000.00 杭州 北京(现货)

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Afizagabar S44819; Egis-13529

产品介绍 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 585nM,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。
生物活性

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.

体外研究

Afizagabar (S44819) is a competitive α5-GABAAR antagonist (Kb=221 nM). Afizagabar selectively inhibits extrasynaptic α5-GABAARs of mouse CA1 pyramidal neurons.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague Dawley (SPRD) rats (In the eight-arm radial maze)
Dosage: 1 and 3 mg/kg
Administration: I.p.
Result: Significantly diminished the marked increase in total errors induced by Scopolamine.
体内研究

Afizagabar (1 and 3 mg/kg; i.p.) significantly diminishes the marked increase in total errors induced by Scopolamine.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague Dawley (SPRD) rats (In the eight-arm radial maze)
Dosage: 1 and 3 mg/kg
Administration: I.p.
Result: Significantly diminished the marked increase in total errors induced by Scopolamine.
性状Solid
溶解性数据
In Vitro: 

DMSO : 6.25 mg/mL (17.11 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7369 mL 13.6844 mL 27.3688 mL
5 mM 0.5474 mL 2.7369 mL 5.4738 mL
10 mM 0.2737 mL 1.3684 mL 2.7369 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

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