Cat. No.: HY-B0113

Omeprazole

(Synonyms: H 16868)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

Omeprazole (H 16868) is an orally active H⁺,K⁺-ATPase inhibitor and a proton pump inhibitor. Omeprazole competitively inhibits CYP2C19, CYP3A4, and CYP2C9 activity. Omeprazole inhibits gastric acid secretion and can be used for acid-related gastrointestinal disorders. Omeprazole inhibits pancreatic cancer cell proliferation, induces apoptosis, autophagosome accumulation (elevated LC3-I and LC3-II levels), oxidative stress, and cytogenetic imbalance, modulates lysosomal transport, reduces inflammatory cytokines. Omeprazole alters small intestinal morphology and magnesium absorption, and induces gastric mucosa morphologic changes. Omeprazole aslo has neuroprotective and antibacterial effects.

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Pureté: 99.96%
CAS No.: 73590-58-6
Formule: C₁₇H₁₉N₃O₃S
Masse moléculaire:345.42

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Omeprazole Chemical Structure

CAS No.: 73590-58-6

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target^[1]^[2]^[5]

CYP2C19

2.4-6.2 μM (Ki)

CYP2C9

16.4 μM (Ki)

CYP3A4

41.9 μM (Ki)

LC3-I

LC3-II

IL-1β

IL-6

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Cellular Effect

Cell Line	Type	Value	Description	References
BXPC-3	IC₅₀	14.8 μM Compound: omeprazole	Inhibition of survival of human BxPC3 cells after 10 to 14 days by crystal violet staining-based colony formation assay Inhibition of survival of human BxPC3 cells after 10 to 14 days by crystal violet staining-based colony formation assay	[PMID: 25513712]
Caco-2	IC₅₀	17.7 μM Compound: Omeprazole	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells	[PMID: 11770010]
HEK293	EC₅₀	14 μM Compound: 1a	Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay Agonist activity at recombinant BRS-3 receptor expressed in baculovirus-transduced HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay	[PMID: 18818070]
HEK-293T	IC₅₀	25 μM Compound: Omeprazole	Inhibition of recombinant human C-MYC/DDK-tagged ENGase expressed in HEK293T cells using heat inactivated bovine ribonuclease B as substrate pretreated for 15 mins followed by substrate addition after 90 mins by SDS-PAGE analysis Inhibition of recombinant human C-MYC/DDK-tagged ENGase expressed in HEK293T cells using heat inactivated bovine ribonuclease B as substrate pretreated for 15 mins followed by substrate addition after 90 mins by SDS-PAGE analysis	[PMID: 28512024]
HepG2	IC₅₀	>10 μM Compound: 92125351	HARVARD: Cytotoxicity in HepG2 cell line HARVARD: Cytotoxicity in HepG2 cell line	[PMID: 22586124]
HepG2	IC₅₀	0.68 μM Compound: 92125351	HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells	[PMID: 22586124]
HUVEC	GI₅₀	>100 μM Compound: Omeprazole	Cytotoxicity against HUVEC cells Cytotoxicity against HUVEC cells	[PMID: 31923859]
K562	GI₅₀	>100 μM Compound: Omeprazole	Antiproliferative activity against human K562 cells harboring MLL1 Antiproliferative activity against human K562 cells harboring MLL1	[PMID: 31923859]
L02	GI₅₀	>100 μM Compound: Omeprazole	Cytotoxicity against human L02 cells Cytotoxicity against human L02 cells	[PMID: 31923859]
MOLM-13	GI₅₀	34.1 μM Compound: Omeprazole	Antiproliferative activity against human MOLM-13 cells harboring MLL1-AF9 Antiproliferative activity against human MOLM-13 cells harboring MLL1-AF9	[PMID: 31923859]
MV4-11	GI₅₀	37.3 μM Compound: Omeprazole	Antiproliferative activity against human MV4-11 cells harboring MLL1-AF4 Antiproliferative activity against human MV4-11 cells harboring MLL1-AF4	[PMID: 31923859]
Vero C1008	CC₅₀	>40 μM Compound: Omeprazole	Cytotoxicity (CC50) determination in Vero E6 cells measured by fluorescence (OD590nm) Cytotoxicity (CC50) determination in Vero E6 cells measured by fluorescence (OD590nm)	10.1101/2020.04.03.023846
Vero C1008	EC₅₀	17.06 μM Compound: Omeprazole	Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days	10.1101/2020.04.03.023846

In Vitro

Omeprazole (15 min) competitively inhibits CYP2C9 activity in pooled human liver microsomes with a K_i of 16.4 μM^[1].
Omeprazole (20 min) competitively inhibits CYP2C19 activity in pooled human liver microsomes with a K_i of 2.4-6.2 μM μM^[1].
Omeprazole (15 min) does not significantly inhibit CYP2D6 activity in pooled human liver microsomes, with an IC₅₀ >200 μM^[1].
Omeprazole (15 min) competitively inhibits CYP3A4 activity in pooled human liver microsomes with a K_i of 41.9 μM^[1].
Omeprazole (0-200 μg/mL; 4 days) inhibits proliferation of MiaPaCa-2, ASPC-1, Panc-1, Colo357, PancTu-1, and Panc89 human pancreatic cancer cell lines in a dose-dependent manner with IC₅₀ values ranging from 9.1 to 42.4 μg/mL^[2].
Omeprazole (80 μg/mL; 30 min-24 ) does not cause consistent intralysosomal pH changes in MiaPaCa-2 and ASPC-1 human pancreatic cancer cell lines, but increases acidity in ASPC-1 cells and decreases acidity in MiaPaCa-2 cells after 24 hours of incubation at 80 μg/mL^[2].
Omeprazole (80-160 μg/mL; 24 h) induces accumulation of early autophagic markers (phagophores and autophagosomes) in MiaPaCa-2 and ASPC-1 human pancreatic cancer cell lines, and induces apoptosis in ASPC-1 cells^[2].
Omeprazole (80 μg/mL; 24 h) accumulates intracellularly in MiaPaCa-2 and ASPC-1 human pancreatic cancer cell lines, and induces changes in fatty acid and phospholipid metabolism^[2].
Omeprazole (80 μg/mL; 24 h) alters the distribution of lysosomal markers and reduces Golgi complex marker expression in MiaPaCa-2 human pancreatic cancer cells, indicating disruption of the lysosomal transport pathway without accumulating in lysosomes or the Golgi complex^[2].
Omeprazole (40-160 μg/mL; 24 h) induces autophagy in a dose-dependent manner with elevated LC3-I and LC3-II levels, and impairs autophagosome turnover in MiaPaCa-2 and ASPC-1 human pancreatic cancer cell lines^[2].
Omeprazole (80 μg/mL; 6-24 h) alters gene expression in ASPC-1 and MiaPaCa-2 human pancreatic cancer cell lines, downregulating bad and survivin and upregulating mdr-1 in ASPC-1 cells^[2].
Omeprazole (80 μg/mL; 24 h) activates autophagy via upregulation of Atg12 in MiaPaCa-2 and ASPC-1 human pancreatic cancer cell lines, and upregulates pro-apoptotic Puma in ASPC-1 cells^[2].
Omeprazole generate sulfone, sulfite
and hydroxy-omeprazole, compounds that can generate more oxidative damage ^[3].
Omeprazole exerts toxicogenic effects in Allium cepa plant cells, as well as Saccharomyces cerevisiae and murine Sarcoma 180 cells^[3].
Omeprazole (200-300 mg/L) results in a
dose-dependent inhibition of E.faecalis at time zero^[6].
Omeprazole (200 mg/L) inhibits S. aureus at both time zero and 2 h^[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[2]

Cell Line:

MiaPaCa-2, ASPC-1, Panc-1, Colo357, PancTu-1, Panc89
Concentration:

0-200 μg/mL
Incubation Time:

4 days
Result:

Inhibited cell proliferation in a dose-dependent manner, with IC₅₀ values of 42.4 μg/mL (MiaPaCa-2), 11.2 μg/mL (ASPC-1), 31.8 μg/mL (Panc-1), 26.4 μg/mL (Colo357), 20.7 μg/mL (PancTu-1), and 9.1 μg/mL (Panc89).
Showed a mild growth-stimulatory hormetic effect in some cell lines at low concentrations.
Mitigated the hormetic growth stimulation induced by low-dose 5-fluorouracil (HY-90006) in ASPC-1, Panc-1, and PancTu-1 cells.
Showed additive effects with low-dose 5-fluorouracil in MiaPaCa-2 cells.
Showed antagonistic effects with low-dose 5-fluorouracil in Panc89 cells.
Showed additive or antagonistic interactions with gemcitabine.

Western Blot Analysis^[2]

Cell Line:

MiaPaCa-2, ASPC-1
Concentration:

40 μg/mL, 80 μg/mL, 160 μg/mL
Incubation Time:

24 h
Result:

Caused a dose-dependent marked elevation of LC3-I and LC3-II fractions in both cell lines.

Real Time qPCR^[2]

Cell Line:

ASPC-1, MiaPaCa-2
Concentration:

80 μg/mL
Incubation Time:

6 h, 12 h, 18 h, 24 h
Result:

Significantly downregulated pro-apoptotic bad mRNA in ASPC-1 cells after 24 hours.
Significantly downregulated pro-survival survivin mRNA in ASPC-1 cells after 24 hours.
Significantly upregulated mdr-1 mRNA in ASPC-1 cells after 24 hours.
Did not significantly alter mdr-1 mRNA expression in MiaPaCa-2 cells.

In Vivo

Omeprazole (20 mg/kg; s.c.; daily; 12-24 weeks) in male Sprague-Dawley rats induces small intestinal inflammation, villous atrophy, tight junction narrowing, and systemic magnesium deficiency with hypomagnesemia^[4].
Omeprazole prevents Oxaliplatin (HY-17371)-induced peripheral neuropathy in Rattus norvegicus^[5].
Omeprazole reduces the levels of the inflammatory cytokines, tumor necrosis factor-α, interleukin-1β, and interleukin-6, in sciatic nerve-ligated mice^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Sprague-Dawley (male, 9 weeks old at study initiation)^[4]
Dosage:

20 mg/kg
Administration:

s.c.; daily; 12 weeks; 24 weeks
Result:

Decreased villous length and mucosa-to-serosa amplification ratio in duodenum, jejunum, and ileum compared to controls.
Increased duodenal crypt depth and width compared to controls.
Reduced the number of secretory granules per Paneth cell in duodenum, jejunum, and ileum after 24 weeks of treatment compared to controls.
Increased CD3+ intraepithelial lymphocytes and CD8+ intraepithelial lymphocytes compared to controls.
Reduced plasma Mg²+ levels to 0.64 mM after 12 weeks and 0.57 mM after 24 weeks compared to control level of 1.07 mmol/L.
Reduced urinary Mg²+ excretion compared to controls.
Increased fecal Mg²+ excretion after 24 weeks of treatment compared to controls.
Reduced bone and muscle Mg²+ content.

Chemical Information

CAS No. 73590-58-6
Appearance Solid
Masse moléculaire 345.42
Formule C₁₇H₁₉N₃O₃S
Color White to off-white
SMILES

O=S(C1=NC2=CC=C(OC)C=C2N1)CC3=NC=C(C)C(OC)=C3C
Synonyms

H 16868
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (10)

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Journal Impact Factor

Cell Metab

Nicotinamide metabolism face-off between macrophages and fibroblasts manipulates the microenvironment in gastric cancer. [Abstract]

2024 Jun 18:S1550-4131(24)00189-X. PMID: 38897198
Cell Host Microbe

Gut-microbiota-derived indole sulfate promotes heart failure in chronic kidney disease. [Abstract]

2025 Oct 8;33(10):1715-1730.e5. PMID: 40961933
Nat Commun

Sequence-based drug design as a concept in computational drug design. [Abstract]

2023 Jul 14;14(1):4217. PMID: 37452028
Adv Sci (Weinh)

CCR7 Mediated Mimetic Dendritic Cell Vaccine Homing in Lymph Node for Head and Neck Squamous Cell Carcinoma Therapy. [Abstract]

2023 Jun;10(17):e2207017. PMID: 37092579
Int J Antimicrob Agents

Expanded applications of omeprazole: Synergistic reversal of colistin resistance in Acinetobacter baumannii. [Abstract]

2025 Oct 8;66(6):107639. PMID: 41072861
Sci Rep

Cysteine-reactive mitigators of small vessel disease-related NOTCH3 mutants. [Abstract]

2026 Mar 20;16(1):14300. PMID: 41862552
J Pharm Biomed Anal

Comprehensive identification and characterization of in vitro and in vivo metabolites of the novel GLP-1 receptor agonist danuglipron using UHPLC-QToF-MS/MS. [Abstract]

2025 Aug 22:267:117128. PMID: 40865303
Br J Clin Pharmacol

Evaluation of a pantoprazole and 4-desmethylpantoprazole-sulfate metabolic ratio as a novel CYP2C19 phenotyping method. [Abstract]

2026 May 31. PMID: 42219154
Tissue Cell

2026 Apr 22:102:103551. PMID: 42033901
Xenobiotica

Notable drug-drug interaction between omeprazole and voriconazole in CYP2C19 *1 and *2 (rs4244285, 681G>A) alleles in vitro. [Abstract]

2024 Oct;54(10):847-854. PMID: 39445918

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (289.50 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

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Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8950 mL

14.4751 mL

28.9503 mL

5 mM

0.5790 mL

2.8950 mL

5.7901 mL

10 mM

0.2895 mL

1.4475 mL

2.8950 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
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Références

[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;32(8):821-827. [Content Brief]

[2]. Udelnow A, et al. Omeprazole inhibits proliferation and modulates autophagy in pancreatic cancer cells. PLoS One. 2011;6(5):e20143. [Content Brief]

[3]. da Mata AMOF, et al. Evaluation of mutagenesis, necrosis and apoptosis induced by omeprazole in stomach cells of patients with gastritis. Cancer Cell Int. 2022;22(1):154. Published 2022 Apr 18. [Content Brief]

[4]. Chamniansawat S, et al. Ultrastructural intestinal mucosa change after prolonged inhibition of gastric acid secretion by omeprazole in male rats. Anat Sci Int. 2021;96(1):142-156. [Content Brief]

[5]. Mori Y, et al. Class effects of proton pump inhibitors in preventing oxaliplatin-induced peripheral neurotoxicity. J Pharmacol Sci. 2025;159(4):279-282. [Content Brief]

[6]. Jonkers D, et al. Omeprazole inhibis growth of Gram-positive and Gram-negative bacteria including Helicobacter pylori in vitro[J]. Journal of Antimicrobial Chemotherapy, 1996, 37(1): 145-150.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8950 mL	14.4751 mL	28.9503 mL	72.3757 mL
	5 mM	0.5790 mL	2.8950 mL	5.7901 mL	14.4751 mL
	10 mM	0.2895 mL	1.4475 mL	2.8950 mL	7.2376 mL
	15 mM	0.1930 mL	0.9650 mL	1.9300 mL	4.8250 mL
	20 mM	0.1448 mL	0.7238 mL	1.4475 mL	3.6188 mL
	25 mM	0.1158 mL	0.5790 mL	1.1580 mL	2.8950 mL
	30 mM	0.0965 mL	0.4825 mL	0.9650 mL	2.4125 mL
	40 mM	0.0724 mL	0.3619 mL	0.7238 mL	1.8094 mL
	50 mM	0.0579 mL	0.2895 mL	0.5790 mL	1.4475 mL
	60 mM	0.0483 mL	0.2413 mL	0.4825 mL	1.2063 mL
	80 mM	0.0362 mL	0.1809 mL	0.3619 mL	0.9047 mL
	100 mM	0.0290 mL	0.1448 mL	0.2895 mL	0.7238 mL

Omeprazole

10 Cited Publications

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Omeprazole

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Activité biologique

Chemical Information

Publications (10)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Omeprazole Related Classifications

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