Bioactivity | 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]. |
CAS | 125598-87-0 |
Sequence | Boc-Trp-Leu-Asp-Phe-NH-NH2 |
Shortening | Boc-WLDF-NH-NH2 |
Formula | C35H47N7O8 |
Molar Mass | 693.79 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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) |