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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.
For research use only. We do not sell to patients.
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[1][2][3][4][5].
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
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
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
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
Omeprazole (15 min) competitively inhibits CYP2C9 activity in pooled human liver microsomes with a Ki of 16.4 μM[1]. Omeprazole (20 min) competitively inhibits CYP2C19 activity in pooled human liver microsomes with a Ki 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 Ki 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.
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.
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.
Room temperature in continental US; may vary elsewhere.
Storage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
Solvent & Solubility
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)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
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
View the Complete Stock Solution Preparation Table
*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.
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.
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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 μLDMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
*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.
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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