A 57696
A 57696 Basic information
- Product Name:
- A 57696
- Synonyms:
-
- A 57696
- Boc-L-Trp-L-Leu-L-Asp-L-Phe-NHNH2
- A57696,A 57696
- L-Phenylalanine, N-[(1,1-dimethylethoxy)carbonyl]-L-tryptophyl-L-leucyl-L-α-aspartyl-, 4-hydrazide (9CI)
- CAS:
- 125598-87-0
- MF:
- C35H47N7O8
- MW:
- 693.8
- Mol File:
- 125598-87-0.mol
A 57696 Chemical Properties
- Boiling point:
- 1081.5±65.0 °C(Predicted)
- Density
- 1.272±0.06 g/cm3(Predicted)
- pka
- 4.20±0.10(Predicted)
A 57696 Usage And Synthesis
Description
A-57696 is a cholecystokinin antagonist. It is selective for cortical CCK-B receptors (IC50 = 25 nM), compared with pancreatic CCK-A receptors (IC50 = 15 microM). It is a competitive antagonist in reversing CCK8-stimulated pancreatic amylase secretion and phosphoinositide breakdown. A-57696 behaved as a partial agonist in stimulating calcium mobilization at CCK-B/gastrin receptors.
Uses
A-57696 is a cholecystokinin antagonist with selective activity at cortical CCK-B receptors (IC50 = 25 nM). A-57696 behaves as a competitive antagonist in reversing CCK8-stimulated pancreatic alpha-amylase secretion and phosphatidylinositol degradation. A-57696 fails to induce gallbladder contraction and inhibits CCK8-induced contraction. A-57696 behaves as a partial agonist at CCK-B/gastrin receptors on NCI-H345 cells, achieving 80% of the maximal CCK8 response. A-57696 and CCK8 inhibit each other in a calcium mobilization assay[1].
References
[1] Distinct requirements for activation at CCK-A and CCK-B/gastrin receptors: studies with a C-terminal hydrazide analogue of cholecystokinin tetrapeptide (30-33) PMID:2601685