加兰他敏 98.9385%(HPLC),分析标准品
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| 包装规格: | 20mg in glass bottle |
| 产品简介: | 一种有效的乙酰胆碱酯酶 (AChE) 抑制剂,IC50 为 500 nM。 |
| 溶解性: | DMSO :≥ 59 mg/mL (205.32 mM) 1M HCl : 50 mg/mL (174.00 mM; ultrasonic and adjust pH to 1 with HCl) |
| 储备液保存: | -80°C, 2 years -20°C, 1 year |
| 体内实验: | 1、请依序添加每种溶剂: 10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (8.70 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2、请依序添加每种溶剂: 10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (8.70 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3、请依序添加每种溶剂: 10% DMSO→90% corn oil Solubility: ≥ 2.5 mg/mL (8.70 mM); Clear solution 此方案可获得 ≥ 2.5 mg/mL (8.70 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 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。 |
| 靶点: | AChE |
| 体外研究: | Galanthamine inhibits AChE and BChE with IC50 of 0.5 and 8.5 μM. Galanthamine acts as a positive allosteric modulator (PAM) of human α4β2 AChRs expressed in permanently transfected HEK 293 cells. Galanthamine increases the response of (α4β2)2α5 AChRs to 1 μM ACh by up to 220% with very low concerntration(EC50=0.25 nM). Only small potentiation (20%) of either α4β2 or (α4β2)2β3 AChRs is detected using FLEXstation assays. Galanthamine at concentrations of 1 μM and above inhibits all three AChR subtypes. |
| 体内研究: | Acute administration of Galantamine (0.3-3 mg/kg, i.p.) increases IGF2 mRNA levels in the hippocampus, but not in the prefrontal cortex, in time- and dose-dependent manner. Galantamine (3 mg/kg, i.p.) causes a transient increase in fibroblast growth factor 2 mRNA levels and a decrease in brain-derived neurotrophic factor mRNA levels in the hippocampus, while it does not affect the mRNA levels of other neurotrophic/growth factors. The Galantamine-induced increase in the hippocampal IGF2 mRNA levels is blocked by Mecamylamine, a nonselective nicotinic acetylcholine (ACh) receptor (nAChR) antagonist, and Methyllycaconitine, a selective α7 nAChR antagonist, but not by Telenzepine, a preferential M1muscarinic ACh receptor antagonist. Moreover, the selective α7 nAChR agonist PHA-543613 increasea the IGF2 mRNA levels, while Donepezil, an acetylcholinesterase inhibitor, does not. Galantamine also increases hippocampal IGF2 protein, which is blocked by Methyllycaconitine. |
| 保存条件: | 2-8℃ |
| 注意事项: | 1、为了您的安全和健康,请穿实验服并戴一次性手套操作。 2、以上信息仅做参考交流之用。 |
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