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130332-27-3

130332-27-3 Structure

130332-27-3 Structure
IdentificationBack Directory
[Name]

4-[[(1R)-2-[[(2R)-3-(1H-INDOL-3-YL)-2-METHYL-1-OXO-2-[[(TRICYCLO[3.3.1.13,7]DEC-2-YLOXY)CARBONYL]AMINO]PROPYL]AMINO]-1-PHENYLETHYL]AMINO]-4-OXOBUTANOIC ACID
[CAS]

130332-27-3
[Synonyms]

[R-(R*,R*)]-4-[[2-[[3-(1H-Indol-3-yl)-2-Methyl-1-oxo-2-[[(tricyclo[3.3.1.13,7]dec-
4-(((R)-2-((R)-2-(((Adamantan-2-yloxy)carbonyl)amino)-3-(1H-indol-3-yl)-2-methylpropanamido)-1-phenylethyl)amino)-4-oxobutanoic acid
4-[[(1R)-2-[[(2R)-3-(1H-INDOL-3-YL)-2-METHYL-1-OXO-2-[[(TRICYCLO[3.3.1.13,7]DEC-2-YLOXY)CARBONYL]AMINO]PROPYL]AMINO]-1-PHENYLETHYL]AMINO]-4-OXOBUTANOIC ACID
Butanoic acid, 4-[[(1R)-2-[[(2R)-3-(1H-indol-3-yl)-2-methyl-1-oxo-2-[[(tricyclo[3.3.1.13,7]dec-2-yloxy)carbonyl]amino]propyl]amino]-1-phenylethyl]amino]-4-oxo-
[Molecular Formula]

C35H42N4O6
[MDL Number]

MFCD09971101
[MOL File]

130332-27-3.mol
[Molecular Weight]

614.73
Chemical PropertiesBack Directory
[storage temp. ]

Store at +4°C
[solubility ]

Soluble to 100 mM in DMSO
[form ]

Powder
Hazard InformationBack Directory
[Uses]

CI-988 is a potent and selective cholecystokinin 2 (CCK-2) receptor antagonist that displays ~ 1600-fold selectivity over CCK1 receptors and has negligible affinity at other binding sites. CI-988 exhibits anxiolytic activity following oral administration. CI-98 inhibited the proliferation of small cell lung cancer (SCLC) cells in mice.
[Biological Activity]

Potent and selective CCK 2 (CCK-B) receptor antagonist that displays ~ 1600-fold selectivity over CCK 1 receptors (IC 50 values are 1.7 and 2717 nM for CCK 2 and CCK 1 respectively). Has negligible affinity at a range of other binding sites (IC 50 > 10 μ M). Exhibits anxiolytic activity following oral administration.
[in vivo]

CI-988 (10 mg/kg; p.o.; daily; for 20 days) inhibits the growth of colorectal cancer in xenografts model mice[3].

Animal Model:Nude mice injected with LoVo cells[3]
Dosage:10 mg/kg
Administration:p.o.; daily; for 20 days
Result:Inhibited the growth of xenografts by 53%.
[storage]

Store at +4°C
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