01
Lansoprazole intermediate 127337-60-4
Product Specification
Appearance: |
White powder |
Identification: |
IR:Similar to reference substance |
Related substance: |
Maximum single impurity NMT0.3%、Total impurity NMT 1.0% |
Loss on drying: |
NMT0.5% |
Assay (HPLC): |
>98% |
description1
PRODUCT DESCRIPTION
2-Chloromethyl-3-methyl-4-(2,2,2-trifluoroethoxy)pyridine Hydrochloride is an intermediate for Lansoprazole (L175000), which is used as a gastric proton pump inhibitor.
Lansoprazole is a proton pump inhibitor that inhibits the H+/K+-ATPase. It inhibits K+ and H+ accumulation in gastric microsomes in a concentration-dependent manner (IC50s = 6.3 and 7.0 μM, respectively) and inhibits H+/K+-ATPase activity by approximately 60% when used at a concentration of 10 μM. Lansoprazole inhibits the H+/K+-ATPase in parietal cells, thus inhibiting gastric acid secretion and increasing intragastric pH. It is a substituted benzimidazole that binds covalently to proton pumps, providing complete and prolonged inhibition of acid secretion. Formulations containing lansoprazole have been used as a proton pump inhibitor and in combination with antibiotics in the treatment of H. pylori infections and duodenal ulcer disease.
H + ,K + -ATPase inhibitor (IC 50 = 6.3 μ M) that displays antisecretory and antiulcer activity. Inhibits gastric acid secretion (IC 50 = 0.09 μ M for histamine-induced acid formation) and reduces gastric lesion formation induced by a variety of ulcerative stimuli. Antibacterial against Helicobacter pylori in vitro . Also blocks swelling-dependent chloride channel (ICIswell) in NIH3T3 fibroblasts. More potent than omeprazole (5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1H-benzimidazole ).
Lansoprazole is a proton pump inhibitor (PPI) similar to omeprazole that inactivates the hydrogen/potassium-stimulated ATPase pumps in parietal cells, thus inhibiting gastric acid secretion and increasing intragastric pH. It is a potent inhibitor of gastric acidity which is widely used in the therapy of gastroesophageal reflux and peptic ulcer disease. Lansoprazole is a racemic mixture of (R)- and (S)-isomers. Dexlansoprazole is an isomer of lansoprazole that has a similar spectrum of activity and toxicities. Lansoprazole therapy is associated with a low rate of transient and asymptomatic serum aminotransferase elevations and is a reported, but very rare cause of clinically apparent liver injury.
Lansoprazole's plasma elimination half-life is not proportional to the duration of the drug's effects (i. e. gastric acid suppression). The plasma elimination half-life is 1. 5 hours or less, and the effects of the drug last for over 24 hours after it has been given for 5 days or more.
Lansoprazole is a prescription medicine used to treat:
● gastroesophageal reflux disease (GERD)
● erosive esophagitis
● stomach ulcers
● duodenal ulcers
● H. Pylori infections
● Zollinger-Ellison syndrome
● gastroesophageal reflux disease (GERD)
● erosive esophagitis
● stomach ulcers
● duodenal ulcers
● H. Pylori infections
● Zollinger-Ellison syndrome