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Butabindide oxalate
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Chemical Name:(2S)-[1-[(2S)-2-amino-1-oxobutyl]-N-butyl]-2,3-dihydro-
1H-indole-2-carboxamide oxalate
Biological Activity:
Potent, reversible, selective and competitive inhibitor of a
CCK-inactivating serine peptidase (tripeptidyl peptidase II) (Ki = 7
nM). Active in vivo (ID50 = 1.1 and 6.8 mg/kg i.v. for inhibition of
liver and brain enzyme respectively).
Roseet al (1996) Characterization and inhibition of a
cholecystokinin-inactivating serine peptidase. Nature 380 403. Rennet al (1998) Characterization and cloning of tripeptidyl peptidase II
from the fruit fly, Drosophila melanogaster. J.Biol.Chem. 273
19173. Ganellinet al (2000) Inhibitors of tripeptidyl peptidase
II. 2. Generation of the first novel lead inhibitor of
cholecystokinin-8-inactivating peptidase: a strategy for the design of
peptidase inhibitors. J.Med.Chem. 43 664.
Inhibitor of dipeptidyl peptidase IV (DPP-IV) (IC50 = 104 nM) that displays selectivity over enzymes with DPP-like activity (IC50 > 30 μM). Increases plasma GLP-1 levels and improves glucose tolerance in diabetic mice following oral glucose challenge.