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Chemical Structure| 161973-10-0 Chemical Structure| 161973-10-0

Structure of Esomeprazole Magnesium
CAS No.: 161973-10-0

Chemical Structure| 161973-10-0

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Esomeprazole magnesium is a proton pump inhibitor for the treatment of gastric acid secretion.

Synonyms: (S)-Omeprazole magnesium; NEXIUM; (–)-Omeprazole Magnesium

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Product Details of Esomeprazole Magnesium

CAS No. :161973-10-0
Formula : C34H36MgN6O6S2
M.W : 713.12
SMILES Code : COC1=C(C)C(CS2=O[Mg+2]3([N]4=C2[N-]C5=C4C=CC(OC)=C5)O=S(CC6=NC=C(C)C(OC)=C6C)C7=[N]3C8=C(C=C(C=C8)OC)[N-]7)=NC=C1C
Synonyms :
(S)-Omeprazole magnesium; NEXIUM; (–)-Omeprazole Magnesium
MDL No. :MFCD06798050

Safety of Esomeprazole Magnesium

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Description
Esomeprazole magnesium ((S)-Omeprazole magnesium) is a potent orally active inhibitor of H+, K+-ATPase, offering therapeutic potential for research into upper intestinal disorders and gastroesophageal reflux disease[1].[2].
Target
  • Proton Pump

In Vitro:

Cell Line
Concentration Treated Time Description References
Human microvascular endothelial cells (HMVECs) 3–100 μM 24 hours To study the effect of omeprazole on DDAH1 and DDAH2 protein expression, results showed omeprazole did not regulate the expression of DDAH1 or DDAH2 Circulation. 2013 Aug 20;128(8):845-53
Human microvascular endothelial cells (HMVECs) 20 μM 24 hours To study the effect of PPIs on intracellular ADMA concentration, results showed PPIs increased intracellular ADMA by ~30% Circulation. 2013 Aug 20;128(8):845-53
RAW 264.7 cells 5-200 μM 24 hours To evaluate the effect of different V-ATPase inhibitors on macrophage uptake of targeted or non-targeted lipid vesicles. ESO pretreatment significantly reduced the endocytosis of both targeted and non-targeted vesicles by macrophages. Int J Nanomedicine. 2020 Aug 25;15:6385-6399
LNCaP cells 140 µM 24 and 48 hours To evaluate the effect of Esomeprazole on LNCaP cell viability and extracellular pH. Results showed that Esomeprazole only caused cell death at the highest concentration and increased extracellular pH from 6.5 to 6.95. Cancers (Basel). 2022 Oct 7;14(19):4916
PC3 cells 140 µM 24 and 48 hours To evaluate the effect of Esomeprazole on PC3 cell viability and extracellular pH. Results showed that Esomeprazole caused 50% cell death after 48 hours and increased extracellular pH from 6.8 to 7.1. Cancers (Basel). 2022 Oct 7;14(19):4916

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice A549 tumor model Intravenous injection 3 mg/kg Single dose, vesicles injected 24 hours later To evaluate the effect of ESO pretreatment on the biodistribution of nanocarriers. ESO pretreatment significantly reduced the liver and spleen distribution of targeted vesicles and enhanced their accumulation in tumors. Int J Nanomedicine. 2020 Aug 25;15:6385-6399
Athymic nude mice PC3 prostate cancer subcutaneous and orthotopic models Gavage 2.5 mg/kg body weight Every other day for three weeks To evaluate the effect of Esomeprazole on tumor growth and acidosis in PC3 prostate cancer models. Results showed that acute administration increased tumor pH from 6.86 to 7.05 after 3 hours, but long-term treatment did not significantly alter tumor growth or acidosis. Cancers (Basel). 2022 Oct 7;14(19):4916
Mice Radiation-induced brain injury model Intraperitoneal injection 10 mg/kg Once daily for 8 weeks Inhibiting the enzymatic activity of AEP to alleviate radiation-induced brain injury iScience. 2024 Apr 9;27(5):109698
Mice Cotton smoke-induced lung injury model Oral 30 mg/kg and 300 mg/kg Daily administration for 21 days To evaluate the prophylactic and therapeutic potential of esomeprazole in a mouse model of cotton smoke-induced lung injury. Results showed that therapeutic esomeprazole significantly inhibited the progression of fibrosis and reduced circulating markers of inflammation and fibrosis. Front Pharmacol. 2017 Jan 26;8:16

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00443963 Dyspepsia PHASE4 WITHDRAWN 2025-12-06 Washington Hospital Center, Wa... More >>shington, District of Columbia, 20010, United States Less <<
NCT00637559 Barrett's Esophagus PHASE4 COMPLETED 2025-04-03 -
NCT01135472 Healthy PHASE1 COMPLETED 2025-04-12 City of Hope Medical Center, D... More >>uarte, California, 91010, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.40mL

0.28mL

0.14mL

7.01mL

1.40mL

0.70mL

14.02mL

2.80mL

1.40mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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