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Omeprazole (H 16868)

Cat. No. M1834
Omeprazole (H 16868) Structure
Synonym:

H 16868; Omeprazol

Size Price Availability Quantity
Free Sample (1-2 mg)  USD 0 In stock
50mg USD 42  USD42 In stock
100mg USD 54  USD54 In stock
500mg USD 88  USD88 In stock
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Quality Control & Documentation
Biological Activity

Omeprazole (H 16868) is a first-in-class proton pump inhibitor (PPI), used for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor). Omeprazol can be used in the treatment of dyspepsia, peptic ulcer disease (PUD), gastroesophageal reflux disease (GORD/GERD), laryngopharyngeal reflux (LPR) and Zollinger–Ellison syndrome. Proton pump inhibitors may be associated with a greater risk of osteoporosis related fractures and Clostridium difficile-associated diarrhea. Proton pump inhibitors (especially omeprazole) have been associated with several cases of acute tubulointerstitial nephritis, an inflammation of the kidneys that often occurs as an adverse compound reaction.

Chemical Information
Molecular Weight 345.42
Formula C17H19N3O3S
CAS Number 73590-58-6
Solubility (25°C) DMSO 80 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] Rezin et al. Basic Clin Pharmacol Toxicol. Gastrin-releasing peptide receptor antagonist or N-acetylcysteine combined with omeprazol protect against mitochondrial complex II inhibition in a rat model of gastritis.

[2] Serebrova et al. Eksp Klin Gastroenterol. Omeprazol and ezomeprazol pharmacokinetics, duration of antisecretory effect, and reasons for their probable changes in duodenal ulcer.

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Keywords: Omeprazole (H 16868), H 16868; Omeprazol supplier, Proton Pump, inhibitors, activators


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