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Esomeprazole Sodium

Cat. No. M3448
Esomeprazole Sodium Structure
Synonym:

(S)-Omeprazole sodium

Size Price Availability Quantity
5mg USD 40  USD40 In stock
10mg USD 60  USD60 In stock
50mg USD 120  USD120 In stock
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Quality Control & Documentation
Biological Activity

Esomeprazole sodium (Nexium) is a sodium salt of esomeprazole that is a potent proton pump inhibitor with an IC50 of 0.076 mg/kg. Esomeprazole sodium (Nexium) suppresses gastric acid secretion by specific inhibition of the H+/K+-ATPase in the gastric parietal cell. Esomeprazole sodium (Nexium) is used in the treatment of dyspepsia, peptic ulcer disease, gastroesophageal reflux disease and Zollinger-Ellison syndrome. Esomeprazole is the S-enantiomer of omeprazole. The S- and R-isomers of omeprazole are protonated and converted in the acidic compartment of the parietal cell forming the active inhibitor, the achiral sulphenamide. By acting specifically on the proton pump, esomeprazole blocks the final step in acid production, thus reducing gastric acidity. This effect is dose-related up to a daily dose of 20 to 40 mg and leads to inhibition of gastric acid secretion.

Chemical Information
Molecular Weight 367.4
Formula C17H18N3O3S.Na
CAS Number 161796-78-7
Solubility (25°C) DMSO 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shan Jing, et al. Pharmacokinetics and Pharmacodynamics of Esomeprazole/Sodium Bicarbonate Immediate-Release Capsules in Healthy Chinese Volunteers: A Cross-Over, Randomized Controlled Trial

[2] Yuta Yokoya, et al. Cost-utility analysis of a 'vonoprazan-first' strategy versus 'esomeprazole- or rabeprazole-first' strategy in GERD

[3] Janusz A Z Jankowski, et al. Esomeprazole and aspirin in Barrett's oesophagus (AspECT): a randomised factorial trial

[4] Qian Qi, et al. Comparative effectiveness and tolerability of esomeprazole and omeprazole in gastro-esophageal reflux disease: A systematic review and meta-analysis

[5] Y Sakurai, et al. Acid-inhibitory effects of vonoprazan 20 mg compared with esomeprazole 20 mg or rabeprazole 10 mg in healthy adult male subjects--a randomised open-label cross-over study

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  Catalog
Abmole Inhibitor Catalog




Keywords: Esomeprazole Sodium, (S)-Omeprazole sodium supplier, Proton Pump, inhibitors, activators


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