130332-27-3
Chemical Structure
CI-988
Synonym(s): PD134308
- CAS No.: 130332-27-3
- Formula:C35H42N4O6
- Molecular Weight:614.73
IUPAC Name: 4-(((R)-2-((R)-2-(((((1R,3S,5R,7R)-adamantan-2-yl)oxy)carbonyl)amino)-3-(1H-indol-3-yl)-2-methylpropanamido)-1-phenylethyl)amino)-4-oxobutanoic acid
InChIKey: FVQSSYMRZKLFDR-QRCSZXLUSA-N
SMILES: OC(CCC(N[C@H](C1=CC=CC=C1)CNC([C@](CC2=CNC3=C2C=CC=C3)(C)NC(OC4[C@H]5C[C@H](C6)C[C@@H]4C[C@H]6C5)=O)=O)=O)=O
Biological Activity: CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects[1][2][3].
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CI-988 | CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects. | |||||||||||||||||||||
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- [1]. Terry W Moody, et al. CI-988 Inhibits EGFR Transactivation and Proliferation Caused by Addition of CCK/Gastrin to Lung Cancer Cells. J Mol Neurosci. 2015 Jul;56(3):663-72. [Content Brief]
- [2]. J Hughes, et al. Development of a class of selective cholecystokinin type B receptor antagonists having potent anxiolytic activity. Proc Natl Acad Sci U S A. 1990 Sep;87(17):6728-32. [Content Brief]
- [3]. R Romani, et al. Gastrin receptor antagonist CI-988 inhibits growth of human colon cancer in vivo and in vitro. Aust N Z J Surg. 1996 Apr;66(4):235-7. [Content Brief]
Keywords
