185213-03-0

Butabindide is a potent inhibitor of cholecystokinin-inactivating peptidase/tripeptidyl peptidase 2 (CCK-inactivating peptidase/TPP-2; K_i = 7 nM). It is selective for CCK-inactivating peptidase/TPP-2 over a panel of serine proteases (K_is = >1 μM) as well as CCK receptors (K_is = >0.1 mM). Butabindide (0.1-100 μM) increases levels of CCK octapeptide (Item Nos. 24404 | 23371) in depolarized rat cerebral cortex slices. In vivo, butabindide inhibits CCK-inactivating peptidase/TPP-2 in mouse liver and brain (ID₅₀s = 1.1 and 6.8 mg/kg, respectively). It also enhances CCK octapeptide-induced delay in gastric emptying and reduces food intake in mice.

Butabindide (UCL-1397) oxalate is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide oxalate inhibits TPP II to protect CCK-8 against inactivation[1][2].

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[1] Ganellin CR, et, al. Inhibitors of tripeptidyl peptidase II. 3. Derivation of butabindide by successive structure optimizations leading to a potential general approach to designing exopeptidase inhibitors. J Med Chem. 2005 Nov 17;48(23):7333-42. DOI:10.1021/jm0500830
[2] Rose C, et, al. Characterization and inhibition of a cholecystokinin-inactivating serine peptidase. Nature. 1996 Apr 4;380(6573):403-9. DOI:10.1038/380403a0