Lansoprazole (AG 1749) 是质子泵抑制剂

Lansoprazole  (Synonyms: 兰索拉唑; AG-1749)

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)。

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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].

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].

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.

分子量    
369.36

性状    
Solid

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

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
 

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. [Content Brief] [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. [Content Brief] [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.  [Content Brief] [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.  [Content Brief] [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.  [Content Brief]