For research use only. Not for therapeutic Use.
CCK-B Receptor Antagonist 2 (CAT: I017593) is a potent, orally active antagonist of the gastrin/cholecystokinin-B (CCK-B) receptor with subnanomolar potency (IC₅₀ = 0.43 nM). It also shows weaker inhibition of CCK-A receptor activity (IC₅₀ = 1.82 μM), demonstrating high selectivity for CCK-B. In vivo, intravenous administration (0.1 μmol/kg) suppresses pentagastrin-induced gastric acid secretion in anesthetized rats with an ED₅₀ of 8.3 nmol/kg. This compound serves as a valuable pharmacological tool for investigating gastrin/CCK-B–mediated signaling, gastric acid regulation, and gastrointestinal pathophysiology, as well as a promising lead for drug discovery in gastric and neurological disorders.
CAS Number | 155412-88-7 |
Synonyms | 1-(3-aminophenyl)-3-[(3R)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-pyridin-2-yl-3H-1,4-benzodiazepin-3-yl]urea |
Molecular Formula | C27H28N6O3 |
Purity | ≥95% |
IUPAC Name | 1-(3-aminophenyl)-3-[(3R)-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-5-pyridin-2-yl-3H-1,4-benzodiazepin-3-yl]urea |
InChI | InChI=1S/C27H28N6O3/c1-27(2,3)22(34)16-33-21-13-5-4-11-19(21)23(20-12-6-7-14-29-20)31-24(25(33)35)32-26(36)30-18-10-8-9-17(28)15-18/h4-15,24H,16,28H2,1-3H3,(H2,30,32,36)/t24-/m0/s1 |
InChIKey | ABJHMASUFPDZRW-DEOSSOPVSA-N |
SMILES | CC(C)(C)C(=O)CN1C2=CC=CC=C2C(=NC(C1=O)NC(=O)NC3=CC=CC(=C3)N)C4=CC=CC=N4 |
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