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Esomeprazole Magnesium trihydrate

Proton pump inhibitor CAS# 217087-09-7

Esomeprazole Magnesium trihydrate

2D Structure

Catalog No. BCC1559----Order now to get a substantial discount!

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Esomeprazole Magnesium trihydrate

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Chemical Properties of Esomeprazole Magnesium trihydrate

Cas No. 217087-09-7 SDF Download SDF
PubChem ID 71316429 Appearance Powder
Formula C34H42MgN6O9S2 M.Wt 767.17
Type of Compound N/A Storage Desiccate at -20°C
Synonyms (S)-Omeprazole magnesium trihydrate
Solubility DMSO : 50 mg/mL (65.17 mM; Need ultrasonic)
Chemical Name magnesium;5-methoxy-2-[(R)-(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]benzimidazol-1-ide;trihydrate
SMILES CC1=CN=C(C(=C1OC)C)CS(=O)C2=NC3=C([N-]2)C=CC(=C3)OC.CC1=CN=C(C(=C1OC)C)CS(=O)C2=NC3=C([N-]2)C=CC(=C3)OC.O.O.O.[Mg+2]
Standard InChIKey VEVZQDGATGBLIC-OWYJLTIPSA-N
Standard InChI InChI=1S/2C17H18N3O3S.Mg.3H2O/c2*1-10-8-18-15(11(2)16(10)23-4)9-24(21)17-19-13-6-5-12(22-3)7-14(13)20-17;;;;/h2*5-8H,9H2,1-4H3;;3*1H2/q2*-1;+2;;;/t2*24-;;;;/m11..../s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Esomeprazole Magnesium trihydrate

DescriptionEsomeprazole Magnesium trihydrate is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells. IC50 value: Target: proton pump Esomeprazole sodium (Nexium) is the S-isomer of omeprazole and acts as a proton pump inhibitor and gastric antisecretory agent indicated for the short-term treatment of gastroesophageal reflux disease in patients with a history of erosive esophagitis. Esomeprazole 0.4 and 0.8 mg/mL as the sodium salt in the infusion solutions tested is chemically and physically stable for at least 2 days at room temperature and 5 days under refrigeration.

References:
[1]. Sandstr?m M, Davidson G, Tolia V et al. Phase I, multicenter, randomized, open-label study evaluating the pharmacokinetics and safety profile of repeated once-daily doses of intravenous esomeprazole in children 0 to 17 years of age. Clin Ther. 2012 Aug;34(8):1828-38. [2]. Wang-Smith L, Fort J, Zhang Y, Sostek M. Pharmacokinetics and relative bioavailability of a fixed-dose combination of enteric-coated naproxen and non-enteric-coated esomeprazole magnesium. J Clin Pharmacol. 2012 May;52(5):670-80. [3]. Johnson TJ, Hedge DD. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9. [4]. Esomeprazole

Esomeprazole Magnesium trihydrate Dilution Calculator

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Esomeprazole Magnesium trihydrate Molarity Calculator

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Preparing Stock Solutions of Esomeprazole Magnesium trihydrate

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.3035 mL 6.5175 mL 13.0349 mL 26.0698 mL 32.5873 mL
5 mM 0.2607 mL 1.3035 mL 2.607 mL 5.214 mL 6.5175 mL
10 mM 0.1303 mL 0.6517 mL 1.3035 mL 2.607 mL 3.2587 mL
50 mM 0.0261 mL 0.1303 mL 0.2607 mL 0.5214 mL 0.6517 mL
100 mM 0.013 mL 0.0652 mL 0.1303 mL 0.2607 mL 0.3259 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Esomeprazole Magnesium trihydrate

Esomeprazole Magnesium (Nexium) is a proton pump inhibitor to reduce gastric acid secretion. The stability of Esomeprazole Magnesium is a function of pH; it rapidly degrades in acidic media, but it has acceptable stability under alkaline conditions. At pH 6.8 (buffer), the half-life of the magnesium salt is about 19 hours at 25°C and about 8 hours at 37°C. Recent randomized controlled trials in patients who are at moderately increased risk of ulcers have shown that the proton pump inhibitor Esomeprazole (the S-isomer of racemic omeprazole) reduces the gastroduodenal ulcer incidence by approximately 70-85% and the gastrointestinal bleeding risk by as much as 90%.

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References on Esomeprazole Magnesium trihydrate

A comparative study of the novel spectrophotometric methods versus conventional ones for the simultaneous determination of Esomeprazole magnesium trihydrate and Naproxen in their binary mixture.[Pubmed:26162342]

Spectrochim Acta A Mol Biomol Spectrosc. 2015;151:538-46.

Two novel simple, specific, accurate and precise spectrophotometric methods manipulating ratio spectra are developed and validated for simultaneous determination of Esomeprazole Magnesium trihydrate (ESO) and Naproxen (NAP) namely; absorbance subtraction and ratio difference. The results were compared to that of the conventional spectrophotometric methods namely; dual wavelength and isoabsorptive point coupled with first derivative of ratio spectra and derivative ratio. The suggested methods were validated in compliance with the ICH guidelines and were successfully applied for determination of ESO and NAP in their laboratory prepared mixtures and pharmaceutical preparation. No preliminary separation steps are required for the proposed spectrophotometeric procedures. The statistical comparison showed that there is no significant difference between the proposed methods and the reported method with respect to both accuracy and precision.

Direct HPLC enantioseparation of omeprazole and its chiral impurities: application to the determination of enantiomeric purity of esomeprazole magnesium trihydrate.[Pubmed:20338705]

J Pharm Biomed Anal. 2010 Sep 5;52(5):665-71.

Analytical and semipreparative high-performance liquid chromatography (HPLC) enantioseparation of the proton-pump inhibitor omeprazole (OME) and its potential organic chiral impurities were accomplished on the immobilised-type Chiralpak IA chiral stationary phase (CSP) under both polar organic and normal-phase conditions. The (S)-enantiomers were isolated with a purity of >99% ee and their absolute configuration was empirically assigned by circular dichroism (CD) spectroscopy. A chemo- and enantioselective HPLC method was validated to control the enantiomeric purity of the (S)-enantiomer of OME (ESO), an active ingredient contained in drug products, in the presence of chiral and achiral related substances. The precision, linearity and accuracy of the determination of the (R)-impurity as well as the recovery of ESO from a pharmaceutical preparation were determined. The proposed method uses the mixture methyl tert-butylether (MtBE)-ethyl acetate (EA)-ethanol (EtOH)-diethylamine (DEA) 60:40:5:0.1 (v/v/v/v) as a mobile phase. In these conditions, linearity over the concentration range 0.5-25 microg/ml for (R)-enantiomer was obtained. The limits of detection and quantification were 99 and 333 ng/ml, respectively. The intra and inter-day assay precision was less than 2% (RSD%).

Description

Esomeprazole Magnesium trihydrate is a proton pump inhibitor which reduces acid secretion through inhibition of the H+ / K+ ATPase in gastric parietal cells.

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