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Lansoprazole intermediate 127337-60-4

IUPAC Name: 2-(chloromethyl)-3-methyl-4-(2,2,2-trifluoroethoxy)pyridine;hydrochloride
Molecular Weight: 276.08
Molecular Formula: C9H9ClF3NO · HCl
Quality Standard: In House

    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