Esomeprazole Sodium

Proton pump inhibitor CAS# 161796-78-7

Esomeprazole Sodium

2D Structure

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Esomeprazole Sodium

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Chemical Properties of Esomeprazole Sodium

Cas No. 161796-78-7 SDF Download SDF
PubChem ID 23708192 Appearance Powder
Formula C17H18N3NaO3S M.Wt 367.4
Type of Compound N/A Storage Desiccate at -20°C
Synonyms (S)-Omeprazole sodium
Solubility DMSO : 250 mg/mL (680.46 mM; Need ultrasonic)
Chemical Name sodium;5-methoxy-2-[(S)-(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1,2-dihydrobenzimidazol-3-ide
SMILES CC1=CN=C(C(=C1OC)C)CS(=O)C2NC3=C([N-]2)C=C(C=C3)OC.[Na+]
Standard InChIKey ALGZIPAMEDTMAM-DPGOWHRRSA-N
Standard InChI InChI=1S/C17H20N3O3S.Na/c1-10-8-18-15(11(2)16(10)23-4)9-24(21)17-19-13-6-5-12(22-3)7-14(13)20-17;/h5-8,17,19H,9H2,1-4H3;/q-1;+1/t17?,24-;/m0./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 Sodium

DescriptionEsomeprazole sodium 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]. Johnson TJ, Hedge DD. Esomeprazole: a clinical review. Am J Health Syst Pharm. 2002 Jul 15;59(14):1333-9. [3]. Thomas C Kupiec, Vasileios Aloumanis, Michel Ben, et al. Physical and Chemical Stability of Esomeprazole Sodium Solutions. Ann Pharmacother. September 2008 ,42 ( 9 ):1247-1251. [4]. Esomeprazole

Esomeprazole Sodium Dilution Calculator

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Esomeprazole Sodium Molarity Calculator

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Preparing Stock Solutions of Esomeprazole Sodium

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.7218 mL 13.6091 mL 27.2183 mL 54.4366 mL 68.0457 mL
5 mM 0.5444 mL 2.7218 mL 5.4437 mL 10.8873 mL 13.6091 mL
10 mM 0.2722 mL 1.3609 mL 2.7218 mL 5.4437 mL 6.8046 mL
50 mM 0.0544 mL 0.2722 mL 0.5444 mL 1.0887 mL 1.3609 mL
100 mM 0.0272 mL 0.1361 mL 0.2722 mL 0.5444 mL 0.6805 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 Sodium

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.

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References on Esomeprazole Sodium

Physical and chemical stability of esomeprazole sodium solutions.[Pubmed:18614750]

Ann Pharmacother. 2008 Sep;42(9):1247-51.

BACKGROUND: Esomeprazole Sodium (Nexium IV, AstraZeneca) is the S-isomer of omeprazole and acts as a proton pump inhibitor gastric antisecretory agent indicated for the short-term treatment of gastroesophageal reflux disease in patients with a history of erosive esophagitis. Currently, there is no information on the long-term stability of Esomeprazole Sodium in infusion solutions beyond 12 hours. OBJECTIVE: To evaluate the stability of Esomeprazole Sodium in 5% dextrose, 0.9% sodium chloride, and lactated Ringer's injection, at 2 concentrations, at room temperature and when refrigerated. METHODS: Triplicate samples of esomeprazole 0.4 and 0.8 mg/mL as the sodium salt were prepared in the solutions required. Stability evaluations were performed initially, over 2 days stored at 23 degrees C, and over 5 days stored at 4 degrees C. Physical stability was assessed using turbidimetric and particulate measurement, as well as visual observation. Chemical stability was evaluated by stability-indicating high-performance liquid chromatography. RESULTS: The samples in all 3 infusion solutions were physically stable throughout the study. None of the samples had evidence of visible haze or particulates. Most samples developed a slight yellow discoloration within 24 hours, but this discoloration was not accompanied by an excessive loss of drug content. The Esomeprazole Sodium samples in all 3 infusion solutions exhibited less than 7% loss over 2 days at 23 degrees C and over 5 days at 4 degrees C. CONCLUSIONS: 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.

Effects of intravenously administered esomeprazole sodium on gastric juice pH in adult female horses.[Pubmed:21457324]

J Vet Intern Med. 2011 May-Jun;25(3):558-62.

BACKGROUND: Gastric ulcers are common in horses and treatment of horses that cannot be administered oral medication can be problematic. OBJECTIVES: To evaluate the efficacy of Esomeprazole Sodium administered intravenously on gastric juice pH and gastric ulcer scores in horses. ANIMALS: Twelve adult female Quarter Horses. METHODS: Esomeprazole Sodium (0.5 mg/kg IV) was administered once daily to 8 horses (treatment group) and saline (5 mL IV) was administered to 4 horses (control group) for 13 consecutive days. Gastroscopy was performed and gastric juice pH and gastric ulcer score were recorded before and 1 hour after the administration of Esomeprazole Sodium or saline on days 1 and 5, then on day 14, 23 hours after the 13th daily dose of Esomeprazole Sodium or saline. RESULTS: When compared with values before treatment, gastric juice pH was higher in Esomeprazole Sodium-treated horses after treatment (4.25 +/- 2.39 versus 6.43 +/- 1.18; P = .002). Also, gastric juice pH was higher (P = .001) in Esomeprazole Sodium-treated horses compared with saline-treated control horses on day 5 and on day 14 values. Gastric ulcers were seen in 5/12 (43%) horses in the study. CONCLUSIONS AND CLINICAL IMPORTANCE: Esomeprazole Sodium shows promise for treatment of gastric ulcers in horses with signs of dysphagia, gastric reflux, or other conditions that restrict oral intake of the current Federal Drug Administration-approved omeprazole paste.

Description

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

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