Omeprazole
(Synonyms: 奥美拉挫; H 16868) 目录号 : GC13166
Omeprazole是一种胃H+/K+ ATPase的抑制剂（PPI），对于猪ATPase的IC50值为1.1μM。Omeprazole对CYP2C19活性具有竞争性抑制作用，抑制常数（Ki）为2至6μM。
Cas No.:73590-58-6
Sample solution is provided at 25 µL, 10mM.
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Omeprazole is an inhibitor of gastric H+/K+ ATPase (PPI) with an IC50 value of 1.1μM for porcine ATPase. Omeprazole has competitive inhibitory effects on CYP2C19 activity with an inhibition constant (Ki) of 2 to 6μM [1-2]. Omeprazole can inhibit the growth of Gram-positive and Gram-negative bacteria [3]. Omeprazole can be used to treat duodenal and gastric ulcers, gastroesophageal reflux disease, and erosive esophagitis [4].
In vitro, Omeprazole (0.1, 1, 2, and 4μg/ml; 3 and 12 days) treatment significantly reduced the expression of CTR, c-fos, NFATc1, and MMP-9 in osteoclasts and osteoblasts (RAW264.7 and MC3T3-E1), regardless of the Omeprazole concentration. With the increase in Omeprazole concentration, the expression of osteocalcin and the ratio of OPG/RANKL in osteoblasts increased [5]. Omeprazole (0-300μM; 7 days) disrupted the morphology and inhibited proliferation of HK2, HPC, and HEK293T cells in a concentration-dependent manner, but had little effect on NRK cells [6].
In vivo, Omeprazole (20mg/kg/day; 2 weeks; oral) treatment improved the movement of mice in a gastric and intestinal disease model induced by hydrochloric acid cysteamine and reduced anxiety behavior [4]. Omeprazole (100mg/kg/day; 1 week; i.p.) treatment increased the bacterial colonization and myeloperoxidase (MPO) activity in the stomach of mice with Helicobacter pylori infection, and increased the expression of anti-apoptotic Bcl-2 protein in the gastric mucosa [7].
References:
[1] Smolka, A.J., Goldenring, J.R., Gupta, S., et al. Inhibition of gastric H,K-ATPase activity and gastric epithelial cell IL-8 secretion by the pyrrolizine derivative ML 3000. BMC Gastroenterol. 4(4), 1-11 (2004).
[2] Li XQ, Andersson TB, Ahlström M, Weidolf L. 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;32(8):821-827.
[3] Jonkers D, Stobberingh E, Stockbrügger R. Omeprazole inhibits growth of gram-positive and gram-negative bacteria including Helicobacter pylori in vitro. J Antimicrob Chemother. 1996;37(1):145-150.
[4] Rethinavel H S, Selvaraj D B, Balakrishnan S J, et al. Omeprazole treatment manifests anxiolytic effects in a cysteamine hydrochloride induced mouse model of gastrointestinal disorder[J]. Heliyon, 2022, 8(6).
[5] Hyun JJ, Chun HJ, Keum B, et al. Effect of omeprazole on the expression of transcription factors in osteoclasts and osteoblasts. Int J Mol Med. 2010;26(6):877-883.
[6] Xiong Z, Lai Z, Li S, et al. Potential Kidney Risks Associated With Clinical Doses of Omeprazole: In Vivo and In Vitro Studies[J]. Clinical and Experimental Pharmacology and Physiology, 2025, 52(8): e70050.
[7] Maróstica M, Arçari D P, Bartchewsky Jr W, et al. Effects of a one-week treatment with acid gastric inhibitors on Helicobacter pylori-infected mice[J]. Scandinavian journal of gastroenterology, 2007, 42(12): 1404-1412.
Omeprazole是一种胃H+/K+ ATPase的抑制剂（PPI），对于猪ATPase的IC50值为1.1μM。Omeprazole对CYP2C19活性具有竞争性抑制作用，抑制常数（Ki）为2至6μM [1-2]。Omeprazole能抑制革兰氏阳性和革兰氏阴性细菌的生长 [3]。Omeprazole可用于治疗十二指肠和胃溃疡、胃食管反流病和糜烂性食管炎 [4]。
在体外，Omeprazole（0.1, 1, 2和4μg/ml; 3, 12天）治疗显著降低了破骨细胞和成骨细胞（RAW264.7和MC3T3-E1）中CTR、c-fos、NFATc1和MMP-9的表达，而与Omeprazole浓度无关。随着Omeprazole浓度的增加，成骨细胞中骨钙蛋白和OPG/RANKL比值的表达增加 [5]。Omeprazole（0-300μM; 7天）以浓度依赖性方式破坏HK2、HPC和HEK293T细胞的形态并抑制增殖，但对NRK细胞的影响很小 [6]。
在体内，Omeprazole（20mg/kg/day; 2周; oral）治疗改善了盐酸半胱胺诱导的胃肠道疾病模型小鼠的运动并减少了焦虑行为 [4]。Omeprazole（100mg/kg/day; 1周; i.p.）治疗改善了幽门螺杆菌感染的小鼠胃中的细菌定植量和髓过氧化物酶（MPO）活性，提高了胃黏膜中抗细胞凋亡Bcl-2蛋白的表达 [7]。
| Cell experiment [1]: | |
Cell lines | HK2, NRK, 293 T and HPC cells |
Preparation Method | The HK2 cell proliferation culture conditions consisted of 95% F12 + 5% fetal bovine serum (FBS) + penicillin/streptomycin and were maintained in an atmosphere of 95% air and 5% CO2. NRK, 293 T and HPC cells were cultured in 90% Dulbecco's modified Eagle medium (DMEM) + 10% FBS + penicillin/streptomycin. The cells were passaged every 3 days and cultured with Omeprazole in 96-well plates at 37°C. Following a 7-day incubation period, the culture medium was replaced with fresh medium and the CCK-8 reagent was added. After a 2h incubation, absorbance was measured at 450nm using a microplate reader. |
Reaction Conditions | 0-300μM; 7 days |
Applications | Omeprazole disrupted the morphology and inhibited the proliferation of HK2, HPC and HEK293T cells in a concentration-dependent manner, but had little effect on NRK cells. |
| Animal experiment [2]: | |
Animal models | BALB/c mice |
Preparation Method | Four to five months old experimental adult BALB/c mice (N = 24) were randomly divided into four groups namely, (1) control (C) group (N = 6), (2) cysteamine HCl (CystM) group (N = 6), (3) Omeprazole (OMP) group (N = 6) and (4) cysteamine HCl with Omeprazole (CystM + OMP) group (N = 6). The animals were maintained in the standard condition at a temperature of about 22–24°C in 12 hours of light and dark alternative cycles in the animal house, Bharathidasan University. Mice were provided with standard rodent feed and water of free access. The experimental animals in group 2 and 4 received intraperitoneal injection of 60mg of cysteamine HCl per Kg body weight for 3 alternative days. Five days later animals in groups 3 and 4 were given 20mg of Omeprazole per Kg body weight through drinking water. The animals in the control group were given normal drinking water. After two weeks of Omeprazole treatment, experimental mice in all groups were subjected to behavioural tests such as OFT, LDB and EPM for assessing the level of anxiety as described earlier. |
Dosage form | 20mg/kg/day; 2 weeks; oral |
Applications | Omeprazole treatment improved the locomotor activity of mice in the gastric and intestinal disease model induced by hydrosulfanide and reduced anxiety behaviors. |
References: | |
| Cas No. | 73590-58-6 | SDF | |
| 别名 | 奥美拉挫; H 16868 | ||
| 化学名 | 3-(quinolin-4-ylmethylamino)-N-[4-(trifluoromethoxy)phenyl]thiophene-2-carboxamide | ||
| Canonical SMILES | CC1=CN=C(C(=C1OC)C)CS(=O)C2=NC3=C(N2)C=C(C=C3)OC | ||
| 分子式 | C17H19N3O3S | 分子量 | 345.42 |
| 溶解度 | ≥ 17.271mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.895 mL | 14.4751 mL | 28.9503 mL |
| 5 mM | 0.579 mL | 2.895 mL | 5.7901 mL |
| 10 mM | 0.2895 mL | 1.4475 mL | 2.895 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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