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兰索拉唑, 钾转运 ATP 酶抑制剂

Proton Pump Inhibitors
  • CAS编号: 103577-45-3
  • 分子式: C16H14F3N3O2S
  • 分子量: 369.36
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货号 (SKU) 包装规格 是否现货 价格 数量
L408751-1ml
1ml 现货 Stock Image
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Compound libraries (12333)

基本描述

英文别名 A-65006, AG-1749 | 2-((3-methyl-4-(2,2,2-trifluoroethoxy)pyridin-2-yl)methylsulfinyl)-1H-benzo[d]imidazole
规格或纯度 Moligand™, 10mM in DMSO
英文名称 Lansoprazole
生化机理 兰索拉唑(A-65006,AG-1749)是一种质子泵抑制剂(PPI),能与顶细胞 H(+)、K(+)-ATP 酶共价结合。兰索拉唑可防止胃产生胃酸。
储存温度 -80℃储存
运输条件 超低温冰袋运输
作用类型 抑制剂
作用机制 钾转运 ATP 酶抑制剂
产品介绍

Lansoprazole is a ATP4A (H+,K+-ATPase) inhibitor (IC50 = 6.3 μM) that displays antisecretory and antiulcer activity. Inhibits gastric acid secretion (IC50 = 0.09 μM for histamine-induced acid formation) and reduces gastric lesion formation induced by a variety of ulcerative stimuli. Antibacterial against Helicobacter pylori in vitro. Also blocks swelling-dependent chloride channel (ICI swell) in NIH3T3 fibroblasts. Lansoprazole is more potent than omeprazoleA H+,K+-ATPase inhibitor that displays antisecretory activity

Information

Lansoprazole Lansoprazole (A-65006, AG-1749) is a proton-pump inhibitor (PPI) that binds covalently to parietal cell H(+),K(+)-ATPase . Lansoprazole prevents the stomach from producing gastric acid.
In vitro

Lansoprazole inhibits gastric acid secretion via inhibition of gastric hydrogen/potassium adenosine triphosphatase (H+,K(+)-ATPase), an enzyme of the gastric parietal cell membrane that forms part of the proton pump that performs the final step in the acid secretory process. Lansoprazole binds covalently to parietal cell H+,K(+)-ATPase, rendering it nonfunctional and inhibiting the secretion of gastric acid. Lansoprazole is a strong anti-secretory agent that acts on gastric H+/K+-adenosine triphosphatase (H+/K+ ATPase) of parietal cells. Lansoprazole inhibits the increased expression of vascular adhesion molecules, the activation of neutrophils, and the production of pro-inflammatory cytokines from activated endothelial cells. Lansoprazole induces several genes, including phase II detoxifying enzyme (NADPH-ubiquinone oxidoreductase, glutathione S-transferase) and antioxidant stress proteins (HO-1, thioredoxin reductase, and superoxide dismutase) in gastric epithelial cells. Lansoprazole significantly inhibits the production of CINC-1 from stimulated RGM-1 cells with IL-1β. Lansoprazole up-regulates HO-1 expression throughout Nrf2 in rat gastric epithelial cells, and the up-regulated HO-1 has anti-inflammatory effects.

In vivo

Lansoprazole inhibits acute inflammatory reactions as well as intestinal mucosal injuries induced by ischemia-reperfusion or indomethacin administration in rats. Lansoprazole significantly inhibits intestinal injuries induced by ischemia-reperfusion or indomethacin. lansoprazole administered exogenously prevents the small intestine against ischemia-reperfusion or indomethacin-induced damage, the action being dependent on its anti-inflammatory and anti-oxidative responses.
Cell Data

cell lines:A431, HCC827, NCI-H292, NCI-H358, NCI-H23, NCI-H1299, Calu-6 and NCI-H460 cells

Concentrations:

Incubation Time:

Powder Purity:≥95%

产品属性

ALogP 2.8

关联靶点(人)

CYP2C19 Tchem 细胞色素 P450 2C19(Cytochrome P450 2C19) (2 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
PHOSPHO1 Tchem 磷酸乙醇胺/磷酸胆碱磷酸酶(Phosphoethanolamine/phosphocholine phosphatase) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)
MAPT Tclin 微管相关蛋白 tau(Microtubule-associated protein tau) (1 活性数据)
活性类型 活性值-log(M) 作用机制 期刊 参考文献(PubMed IDs)

名称和识别符

分子类型 小分子
Isomeric SMILES CC1=C(C=CN=C1CS(=O)C2=NC3=CC=CC=C3N2)OCC(F)(F)F
分子量 369.36
Reaxy-Rn 4333393
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4333393&ln=

化学和物理性质

熔点 173-175°C

安全和危险性(GHS)

象形图 GHS07
信号词 Warning
危险声明

H315: 引起皮肤刺激

H319: 引起严重眼睛刺激

H335: 可能引起呼吸道刺激

预防措施声明

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾

P305+P351+P338: 如进入眼睛:用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出,取出隐形眼镜。继续冲洗。

P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。

P302+P352: 如皮肤沾染:用水充分清洗。

P321: 特殊处理(请参阅此标签上的...)。

P405: 密闭存放

P501: 将内容物/容器处理到。。。

P264: 处理后要彻底洗手。

P271: 仅在室外或通风良好的地方使用。

P304+P340: 如误吸入:将人转移到空气新鲜处,保持呼吸舒适体位。

P403+P233: 存放在通风良好的地方。保持容器密闭。

P362+P364: 脱掉沾污的衣服,清洗后方可重新使用。

P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。

P337+P317: 如果眼睛刺激持续:寻求医疗帮助。

P332+P317: 如果出现皮肤刺激:请寻求医疗帮助。

P319: 如果你感到不适,请寻求医疗帮助。

WGK Germany 2
RTECS DD9487500
Merck Index 5362
个人防护装备 dust mask type N95 (US), Eyeshields, Gloves

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

此产品的引用文献

引用文献

1. Yuhong Liu, Jiali Liang, Jiazhen Wu, Hanbin Chen, Zhenbiao Zhang, Hongmei Yang, Liping Chen, Haiming Chen, Ziren Su, Yucui Li.  (2017)  Transformation of patchouli alcohol to β-patchoulene by gastric juice: β-patchoulene is more effective in preventing ethanol-induced gastric injury.  Scientific Reports,  (1): (5591).  [PMID:28717228] [10.1038/s41598-017-05996-5]

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