Anatabine dicitrate 是一种烟草生物碱，可以穿过血脑屏障。Anatabine dicitrate 是一种有效的α4β2 nAChR激动剂。Anatabine dicitrate 通过阻止淀粉样蛋白前体蛋白的 β 裂解，抑制NF-κB激活，并降低淀粉样 β (Aβ) 的产生。Anatabine dicitrate 具有抗炎作用，可用于神经退行性疾病的研究。
| 生物活性 | Anatabine dicitrate is a tobacco alkaloid that can cross the blood-brain barrier. Anatabine dicitrate is a potentα4β2nAChRagonist. Anatabine dicitrate inhibitsNF-κBactivation loweramyloid-β(Aβ)production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine dicitrate has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment[1][2][3]. |
| IC50& Target | NF-κB[1]
Amyloid-β (Aβ)[1]
α4β2 nAChR[2] |
体外研究
(In Vitro) | Anatabine (600 μg/mL; 24 hours; SHSY-5Y cells) treatment shows an inhibition of p65 NF-κB phosphorylation[1].
Anatabine (500-1000μg/mL; 30 minutes; SHSY-5Y cells) treatment fully prevents the increase in BACE-1 mRNA levels induced by TNF-α. After 24 hours, Anatabine treatment shows a dose-dependent inhibition of BACE-1 protein levels[1].
Anatabine dose dependently inhibits Aβ1-40and Aβ1-42with an approximate half maximal inhibitory concentration of 640 μg/mL for both Aβ1-40and Aβ1-42in 7W CHO cells. Anatabine inhibits sAPPβ secretion without impacting sAPPα suggesting that Anatabine is preventing the β-cleavage of amyloid precursor protein (APP)[1].
Western Blot Analysis[1] | Cell Line: | SHSY-5Y cells | | Concentration: | 600 μg/mL | | Incubation Time: | 24 hours | | Result: | An inhibition of p65 NF-κB phosphorylation was observed. |
RT-PCR[1] | Cell Line: | SHSY-5Y cells | | Concentration: | 500 μg/mL, 1000 μg/mL | | Incubation Time: | 30 minutes | | Result: | Fully prevented the increase in BACE-1 mRNA levels induced by TNF-α. |
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体内研究
(In Vivo) | Anatabine (0.5-2 mg/kg; intraperitoneal injection; daily; for 4 days; transgenic mouse) treatment significantly lowers brain soluble Aβ1-40and Aβ1-42levels in a transgenic mouse model of Alzheimer's disease[1].
| Animal Model: | Transgenic mice overexpressing the human APP695sw mutation and the presenilin-1 mutation M146L (Tg PS1/APPsw) (50 week-old)[1] | | Dosage: | 0.5 mg/kg, 2 mg/kg | | Administration: | Intraperitoneal injection; daily; for 4 days | | Result: | Significantly lowered brain soluble Aβ1-40and Aβ1-42levels in a transgenic mouse model of Alzheimer's disease. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 100 mg/mL(183.67 mM;Need ultrasonic) DMSO : 30 mg/mL(55.10 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.8367 mL | 9.1834 mL | 18.3668 mL | | 5 mM | 0.3673 mL | 1.8367 mL | 3.6734 mL | | 10 mM | 0.1837 mL | 0.9183 mL | 1.8367 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂： ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂： PBS Solubility: 50 mg/mL (91.83 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
