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[CAS NO. 161973-10-0] Esomeprazole magnesium
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-B1446 |
| Brand: | MCE |
| CAS: | 161973-10-0 |
Overview
| MDL | MFCD06798050 |
|---|---|
| Molecular Weight | 713.12 |
| Molecular Formula | C34H36MgN6O6S2 |
| SMILES | CC1=C(N=CC(C)=C1OC)CS2=O[Mg+2]3([N](C4=CC=C(OC)C=C4[N-]5)=C5S(CC(N=CC(C)=C6OC)=C6C)=O3)[N]7=C2[N-]C8=CC(OC)=CC=C78 |
Summary
Esomeprazole magnesium ((S)-Omeprazole magnesium) is a potent and orally active H + , K + -ATPase inhibitor. Esomeprazole magnesium has the potential for upper intestinal disorders and gastroesophageal reflux disease research [1] [2] . Esomeprazole magnesium acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H + -ATPases [4] .
IC50 & Target
H + , K + -ATPase [1]
In Vitro
Esomeprazole magnesium is an inhibitor of H + , K + -ATPase [1] .Esomeprazole magnesium is develped from Esomeprazole strontium tetrahydrate (EST). EST contains esomeprazole, the S-enantiomer of omeprazole a salt-exchanged version of Esomeprazole magnesium trihydrate [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Esomeprazole magnesium (0.5-50 mg/kg; oral gavage; daily; for 10 days; A/J mice) treatment increases gastric total antioxidant capacity and Cu/Zn-superoxide dismutase activity [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | A/J mice [1] |
| Dosage: | 0.5 mg/kg, 5 mg/kg, 50 mg/kg |
| Administration: | Oral gavage; daily; for 10 days |
| Result: | Gastric total antioxidant capacity and Cu/Zn-superoxide dismutase activity are increased. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02680132 | Torrent Pharmaceuticals Limited |
Healthy
|
May 2011 | Phase 1 |
| NCT00206180 | AstraZeneca |
Erosive Esophagitis|Reflux Esophagitis|Gastroesophageal Reflux Disease
|
June 2004 | Phase 4 |
| NCT01135472 | City of Hope Medical Center |
Healthy
|
March 2010 | Phase 1 |
| NCT00637559 | AstraZeneca |
Barrett´s Esophagus
|
March 2002 | Phase 4 |
| NCT00079833 | AstraZeneca |
Zollinger-Ellison Syndrome
|
November 2003 | Phase 3 |
| NCT02659683 | Torrent Pharmaceuticals Limited |
Healthy Subjects
|
May 2011 | Phase 1 |
| NCT01142128 | University of Florida|AstraZeneca |
Chronic Pancreatitis
|
February 2009 | Phase 1 |
| NCT00443963 | Medstar Health Research Institute|AstraZeneca |
Dyspepsia
|
December 2006 | Phase 4 |
| NCT00637845 | AstraZeneca |
Heartburn|Gastroesophageal Reflux Disease
|
June 2002 | Phase 4 |
| NCT02680119 | Torrent Pharmaceuticals Limited |
Healthy
|
May 2011 | Phase 1 |
| NCT04696783 | Fifth Affiliated Hospital, Sun Yat-Sen University |
Gastroesophageal Reflux Disease
|
July 2021 | Phase 3 |
| NCT00687245 | AstraZeneca |
Endoscopically-Proven GERD|Reflux
|
August 2006 | Phase 1 |
| NCT00474903 | National Cancer Institute (NCI) |
Barrett Esophagus|Esophageal Cancer
|
April 2007 | Phase 2 |
| NCT00206024 | AstraZeneca |
Heartburn
|
November 2004 | Phase 4 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 125 mg/mL ( 175.29 mM )
H 2 O : 3 mg/mL ( 4.21 mM ; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.4023 mL | 7.0114 mL | 14.0229 mL |
| 5 mM | 0.2805 mL | 1.4023 mL | 2.8046 mL |
| 10 mM | 0.1402 mL | 0.7011 mL | 1.4023 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (2.92 mM); Clear solution
-
3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.08 mg/mL (2.92 mM); Clear solution
-
4.
Add each solvent one by one: PBS
Solubility: 1.43 mg/mL (2.01 mM); Clear solution; Need ultrasonic
References
- [1] Timothy R Koch, et al. Effect of the H, K-ATPase inhibitor, esomeprazole magnesium, on gut total antioxidant capacity in mice. J Nutr Biochem. 2004 Sep;15(9):522-6.
- [2] Pankaj Kumar, et al. Preparation and characterization of pH-sensitive methyl methacrylate-g-starch/hydroxypropylated starch hydrogels: in vitro and in vivo study on release of esomeprazole magnesium. Drug Deliv Transl Res. 2015 Jun;5(3):243-56.
- [3] 2013 Annual Meeting. Abstract Supplement
- [4] Huarui Zhang, et al. Advances in the discovery of exosome inhibitors in cancer. J Enzyme Inhib Med Chem. 2020 Dec;35(1):1322-1330.
Synonyms
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