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Omeprazole sodium/奥美拉唑钠 {[allProObj[0].p_purity_real_show]}

货号:A208846 同义名: H 16868 sodium

Omeprazole sodium是一种质子泵(proton pump)抑制剂 (PPI),在胃肠道疾病研究中具有潜力。它竞争性抑制 CYP2C19 的活性。此外,Omeprazole 还能抑制革兰氏阳性菌和革兰氏阴性菌的生长。同时,它也是中性鞘磷脂酶 (N-SMase) 的抑制剂,具有外泌体抑制的作用。

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There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Omeprazole sodium/奥美拉唑钠 化学结构 CAS号:95510-70-6
Omeprazole sodium/奥美拉唑钠 化学结构
CAS号:95510-70-6
Omeprazole sodium/奥美拉唑钠 3D分子结构
CAS号:95510-70-6
Omeprazole sodium/奥美拉唑钠 化学结构 CAS号:95510-70-6
Omeprazole sodium/奥美拉唑钠 3D分子结构 CAS号:95510-70-6
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Omeprazole sodium/奥美拉唑钠 纯度/质量文件 产品仅供科研

货号:A208846 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Proton Pump 其他靶点 纯度
Zinc pyrithione 98+%
PF 03716556 ++++

H+/K+-ATPase, pIC50: ~6.5

99%
Lansoprazole 98%
Esomeprazole Magnesium 98%+
Rabeprazole 99%+
Ilaprazole TOPK 97%
Bafilomycin A1 ++++

H+-ATPase, IC50: 0.44 nM

99%
Pantoprazole sodium 98%
(R)-Lansoprazole 98%
Tenatoprazole 99%+
Omeprazole 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Omeprazole sodium/奥美拉唑钠 生物活性

描述 Omeprazole sodium (H 16868 sodium), another form of this proton pump inhibitor, also targets acid-related gastrointestinal disorders and similarly inhibits CYP2C19 activity with a Ki of 2 to 6 μM[1]. This sodium salt form also restricts the growth of both Gram-positive and Gram-negative bacteria[2]. Omeprazole is a significant inhibitor of neutral sphingomyelinase (N-SMase), impacting brain pathways related to exosome production[3].
体外研究

For treating gastrointestinal disorders, Omeprazole (H 16868) has shown to significantly reduce intragastric acidity, with median 24-hour intragastric pH increasing from 1.4 to 5.3 and mean hourly hydrogen ion activity dropping from 38.50 to 1.95 mmol(mEq)/L, surpassing the effectiveness of cimetidine and ranitidine[1].

The pharmacokinetic behavior of omeprazole was evaluated in healthy male subjects who received either single or repeated doses of 30 and 60 mg. The absorption from its enteric-coated formula proved unpredictable, but a significant increase in the area under the plasma concentration-time curve (AUC) was observed after repeated doses, suggesting enhanced bioavailability, likely due to the compound's ability to inhibit its own gastric acid secretion[2].

Omeprazole sodium is a potent inhibitor of neutral sphingomyelinase (N-SMase), effectively penetrating the brain and impacting exosome regulation[3].

Omeprazole sodium/奥美拉唑钠 细胞实验

Cell Line
Concentration Treated Time Description References
Human peripheral blood mononuclear cells (PBMC) 50 μg/mL 4 and 24 hours Evaluate the inhibitory effect of omeprazole on LPS-induced inflammatory cytokine production, results showed omeprazole inhibited TNF-α, MCP-1, IL-23, and IL-12 production Adv Sci (Weinh). 2022 Jan;9(3):e2104051.
THP-1 cell-derived macrophages 50 μg/mL 4 hours Evaluate the inhibitory effect of omeprazole on TLR4 signaling pathways, results showed omeprazole significantly inhibited NF-κB/AP-1 and IRF activation Adv Sci (Weinh). 2022 Jan;9(3):e2104051.
Mouse fundic organ cultures 80 μmol/ml 12 hours To investigate the effect of Ca2+i chelation on Shh gene expression, results showed that EGTA and BAPTA-AM significantly inhibited Shh expression. Gastroenterology. 2010 Dec;139(6):2061-2071.e2.
Human saphenous vein segments (SV) 3 to 100 μM 24 hours To study the effect of omeprazole on NO production, results showed that omeprazole significantly inhibited NOx release. Circulation. 2013 Aug 20;128(8):845-53.
Human microvascular endothelial cells (HMVECs) 20 μM 24 hours To study the effect of PPIs on ADMA concentration in endothelial cells, results showed that PPIs increased intracellular ADMA by ~30%. Circulation. 2013 Aug 20;128(8):845-53.
RAW264.7 macrophages 50 µM 72 hours Test the protective effect of omeprazole on Mycobacterium tuberculosis-infected macrophages, results showed omeprazole failed to protect macrophages at 50 µM Nat Commun. 2015 Jul 9;6:7659.
MRC-5 lung fibroblasts 50 µM 72 hours Test the protective effect of omeprazole against Mycobacterium tuberculosis-induced cytotoxicity, results showed omeprazole failed to protect fibroblasts at 50 µM Nat Commun. 2015 Jul 9;6:7659.

Omeprazole sodium/奥美拉唑钠 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice Men1ΔIEC; Sst−/− mice Oral 200 ppm chow 6 months to 1 year To study the effect of omeprazole on gastrin expression and menin nuclear export in Men1ΔIEC; Sst?/? mice, results showed omeprazole treatment increased gastrin expression and menin nuclear export. Gastroenterology. 2017 Dec;153(6):1555-1567.e15
Mice Wild-type mice Intraperitoneal injection 400 μmol/kg Once daily for 3 consecutive days To investigate the effect of omeprazole on gastric acid secretion and Shh gene expression, results showed that omeprazole significantly inhibited gastric acid secretion and Shh gene expression. Gastroenterology. 2010 Dec;139(6):2061-2071.e2.
Mice Wild-type C57BL/6 mice Intraperitoneal injection 10 μmol/mouse Single injection, euthanized after 2 hours Omeprazole inhibited gastric acid secretion and reduced Shh expression, with additive effect when combined with IL-1β Gastroenterology. 2010 Feb;138(2):562-72, 572.e1-2
Mice H. pylori infection model Oral gavage 1.5 mg/20 g body weight Once daily for one week To evaluate the effect of omeprazole on the distribution of H. pylori in the stomach. Results showed that omeprazole-mediated acid suppression promoted H. pylori colonization in the proximal and distal corpus but did not alter its distribution within the gastric glands. Gastroenterology. 2019 Jan;156(1):160-174.e7
Mice Men1ΔIEC; Sst−/− mouse model Dietary administration 200 ppm 6 months To investigate the effect of omeprazole on gastric carcinoid development. Results showed that omeprazole treatment accelerated gastric carcinoid formation in Men1ΔIEC; Sst?/? mice, associated with hypergastrinemia. Gut. 2017 Jun;66(6):1012-1021
Mice Gastric mucosal injury model Intraperitoneal injection 60 mg/kg At least 30 minutes before surgery Omeprazole reduced maximal damage size and accelerated epithelial repair, although only at pH 3 did omeprazole further increase surface pH above the level caused by imposed damage. Gut. 2012 Jun;61(6):804-11
Mice Acute esophagitis model Subcutaneous injection 400 μmol/kg Single dose administered 1 hour before surgery Omeprazole significantly reduced MPO activity and pathological damage scores in wild-type mice, similar to the effect of the VR-1 antagonist capsazepine. Gut. 2006 Jan;55(1):34-40
C57BL/6 wild-type male mice LPS-induced acute lung injury (ALI) model Intratracheal injection 75 μg/kg Nano-OM Single dose, samples collected after 24 hours Evaluate the therapeutic effect of nano-omeprazole on ALI, results showed nano-omeprazole reduced inflammatory cell infiltration and cytokine production, protecting the lungs from injury Adv Sci (Weinh). 2022 Jan;9(3):e2104051.
INS-GAS mice H. pylori infection model Oral 400 μmol/kg/d Twice daily for 7 days To evaluate the efficacy of omeprazole combined with antibiotics in preventing the progression of gastric cancer in H. pylori-infected mice. Results showed that early treatment (8 weeks) completely prevented the development of GIN, while treatments at 12 and 22 weeks also significantly reduced the severity of GIN. Cancer Res. 2008 May 1;68(9):3540-8
Male C57BL/6JJcl mice High-fructose diet-induced small intestine injury model Intraperitoneal injection 20 mg/kg Once daily for 9 weeks Omeprazole exacerbated ASA-induced intestinal damage, significantly decreased Bifidobacteria levels, and significantly increased A. muciniphila counts in the jejunum. Gut Microbes. 2020 Sep 2;11(5):1385-1404

Omeprazole sodium/奥美拉唑钠 参考文献

[1]Li XQ, et al. Comparison of inhibitory effects of the proton pump-inhibiting drugs omeprazole, esomeprazole, lansoprazole, pantoprazole, and rabeprazole on human cytochrome P450 activities. Drug Metab Dispos. 2004 Aug;32(8):821-7.

[2]Jonkers D, et al. Omeprazole inhibits growth of gram-positive and gram-negative bacteria including Helicobacter pylori in vitro. J Antimicrob Chemother. 1996 Jan;37(1):145-50.

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

Omeprazole sodium/奥美拉唑钠 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.72mL

0.54mL

0.27mL

13.61mL

2.72mL

1.36mL

27.22mL

5.44mL

2.72mL

Omeprazole sodium/奥美拉唑钠 技术信息

CAS号95510-70-6
分子式C17H18N3NaO3S
分子量 367.4
SMILES Code O=S(C1=NC2=CC=C(OC)C=C2[N-]1)CC3=NC=C(C)C(OC)=C3C.[Na+]
MDL No. MFCD07802816
别名 H 16868 sodium
运输蓝冰
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 120 mg/mL(326.62 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 5.5 mg/mL(14.97 mM),配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
方案 一
方案 二
方案 三
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