Bioactivity | T-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guinea pig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist. |
CAS | 169042-78-8 |
Formula | C28H21FN3NaO5 |
Molar Mass | 521.47 |
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]. Pharmacological profile of T-0632, a novel potent and selective CCK A receptor antagonist, in vitro |