兰索拉唑, 钾转运 ATP 酶抑制剂

Proton Pump Inhibitors
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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 (12332)

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 3.442
hba_count 4
HBD Count 1
Rotatable Bond 6

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
Canonical SMILES CC1=C(OCC(F)(F)F)C=CN=C1C[S](=O)C2=NC3=CC=CC=C3[NH]2
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

DMSO(mg / mL) Max Solubility 74
DMSO(mM) Max Solubility 200.35
Water(mg / mL) Max Solubility <1

安全和危险性(GHS)

Reaxy-Rn 4333393
Reaxys-RN link address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4333393&ln=

技术规格说明书

Concentration(Compounding value) 9.8-10.2(mmol/L)
Appearance(L408751) Colorless Transparent Liquid

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

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]

参考文献

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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