| Identification | Back Directory | [Name]
Carbamic acid,N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]-,methyl ester | [CAS]
158364-59-1 | [Synonyms]
PUMAPRAZOLE
Carbamic acid,N-[2-[[(2,3-dimethylimidazo[1,2-a]pyridin-8-yl)amino]methyl]-3-methylphenyl]-,methyl ester | [Molecular Formula]
C19H22N4O2 | [MDL Number]
MFCD00933297 | [MOL File]
158364-59-1.mol | [Molecular Weight]
338.4 |
| Chemical Properties | Back Directory | [density ]
1.21±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
13.67±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Description]
Pumaprazole has been abandoned
in favor of a pharmacologically better
follow up compound presently under development
at Byk Gulden. The WHO decided to
label the APAs by the stem syllable “-prazole”
in order “to maintain the number of stems at
a manageable level”, irrespective of the completely
different (i.e., reversible vs. covalent)
modes of drug – target interactions by APAs and
PPIs (WHO decision communicated on Nov. 30,
1995). Unfortunately, this pharmacologically
misleading but legally binding decision will confuse
the rational use and differential perception
of APAs vs. PPIs in the future and counteracts
the effort for an unambiguous terminology in
pharmacology. It should be noted that the terms
APAs and PPIs have been coined specifically
to make a clearly recognizable distinction between
the two chemically and mechanistically
different classes of drugs. | [Uses]
Pumaprazole is a reversible proton pump antagonist. | [in vivo]
Pumaprazole is a reversible proton pump antagonist. Basal acid secretion in the Ghosh-Schild rat is inhibited by Pumaprazole with a higher efficacy compare to ranitidine. Pumaprazole displays identical ID50 values on day 1 (11 μmol/kg, 95% confidence limits of 5 and 23) and on day 7 (10 μmol/kg, 95% confidence limits of 4 and 23) of a repeated dose study in this model. The lower dose of Pumaprazole (27 μmol/kg) rapidly elevates luminal pH up to almost neutrality, the higher dose (54 μmol/kg) further prolongs this pH-elevating effect[1]. | [storage]
Store at -20°C | [References]
[1] Kromer W, et al. Animal pharmacology of reversible antagonism of the gastric acid pump, compared to standard antisecretory principles. Pharmacology. 2000 May;60(4):179-87. DOI:10.1159/000028367 |
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