| Identification | Back Directory | [Name]
Butabindide oxalate | [CAS]
185213-03-0 | [Synonyms]
[S-(R*,R*)]-1-(2-Amino-1-oxobutyl)-N-butyl-2,3-dihydro-1H-indole-2-carboxamide ethanedioate | [Molecular Formula]
C19H27N3O6 | [MOL File]
185213-03-0.mol | [Molecular Weight]
393.434 |
| Chemical Properties | Back Directory | [Melting point ]
142 °C | [storage temp. ]
Desiccate at -20°C | [solubility ]
Soluble to 100 mM in water and to 100 mM in DMSO | [form ]
Powder | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
Butabindide is a potent inhibitor of cholecystokinin-inactivating peptidase/tripeptidyl peptidase 2 (CCK-inactivating peptidase/TPP-2; Ki = 7 nM). It is selective for CCK-inactivating peptidase/TPP-2 over a panel of serine proteases (Kis = >1 μM) as well as CCK receptors (Kis = >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. | [Uses]
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]. | [in vivo]
Butabindide (UCL-1397; 10 mg/kg; i.v.; for 20 min) oxalate inhibits the breakdown of CCK-8 in the gastrointestinal tract and increases satiety in mice[2]. | Animal Model: | Mice (25-30 g)[2] | | Dosage: | 10 mg/kg | | Administration: | Intravenous injection; for 20 minutes | | Result: | Reduces food intake and elicits other behavioral concomitants of satiation. |
| [storage]
Desiccate at -20°C | [References]
[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 |
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