Lansoprazole(Synonyms: 兰索拉唑; AG-1749)

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Lansoprazole (Synonyms: 兰索拉唑; AG-1749) 纯度: ≥98.0%

Lansoprazole (AG 1749) 是质子泵抑制剂,能抑制胃酸生成。Lansoprazole (AG 1749) 是中性鞘磷脂酶 (N-SMase) 的抑制剂(外泌体抑制剂)。

Lansoprazole(Synonyms: 兰索拉唑; AG-1749)

Lansoprazole Chemical Structure

CAS No. : 103577-45-3

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生物活性

Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)[1][2].

体外研究
(In Vitro)

Lansoprazole from 0.3 to 3 μM inhibits gastric acid formation in a concentration-dependent manner (IC50 of 0.76 μM)[4].
Lansoprazole (30-300 μM) both induced concentration-dependent, reversible and reproducible relaxations of arteries[5].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Lansoprazole (20-40 mg/kg) treatment significantly attenuated STZ and HFD -induced memory deficits, biochemical and histopathological alterations[3].
Lansoprazole (20 mg/kg and 40 mg/kg, p.o.) significantly reduces the STZ and HFD- induced increase in AChE activity[3].
Lansoprazole (20 mg/kg and 40 mg/kg, p.o.) significantly reduces the STZ and HFD- induced rise in brain MPO level[3].
Further HFD mice treated with lansoprazole (20 mg/kg and 40 mg/kg, p.o.) shows a marked decrease in the body weight in comparison to the control animals[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Swiss albino mice (20–25 g) of either sex[3].
Dosage: 20 mg/kg, 40 mg/kg.
Administration: PO, started after second dose of STZ and then subjected to MWM test. Continued (30 min before) during the acquisition trial conducted from day 1 to day 4.
Result: Significantly attenuated the day 4 rise in ELT and decreased in day 5 TSTQ in the STZ as well as HFD treated mice in a dose dependent manner.

Clinical Trial

分子量

369.36

Formula

C16H14F3N3O2S

CAS 号

103577-45-3

中文名称

兰索拉唑

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
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (270.74 mM; Need ultrasonic)

H2O : 0.1 mg/mL (0.27 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7074 mL 13.5369 mL 27.0739 mL
5 mM 0.5415 mL 2.7074 mL 5.4148 mL
10 mM 0.2707 mL 1.3537 mL 2.7074 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。

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: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.77 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.77 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.77 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。

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Kokufu, T., et al., Effects of lansoprazole on pharmacokinetics and metabolism of theophylline. Eur J Clin Pharmacol, 1995. 48(5): p. 391-5.

    [2]. Huarui Zhang, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330.

    [3]. Rupinder K Sodhi, et al. Defensive effect of lansoprazole in dementia of AD type in mice exposed to streptozotocin and cholesterol enriched diet. PLoS One. 2013 Jul 31;8(7):e70487.

    [4]. Jun Matsukawa, et al. A comparative study on the modes of action of TAK-438, a novel potassium-competitive acid blocker, and lansoprazole in primary cultured rabbit gastric glands. Biochem Pharmacol. 2011 May 1;81(9):1145-51.

    [5]. Erdinc Naseri, et al. Proton pump inhibitors omeprazole and lansoprazole induce relaxation of isolated human arteries. Eur J Pharmacol. 2006 Feb 15;531(1-3):226-31.

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