T-0632 

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.

521.47

C₂₈H₂₁FN₃NaO₅

169042-78-8

O=C(O[Na])CC[C@@]1(NC(C2=CC3=C(C=N2)C=CC=C3)=O)C(N(C4=CC=CC=C4F)C5=C1C=CC(OC)=C5)=O

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• [1]. Pharmacological profile of T-0632, a novel potent and selective CCK A receptor antagonist, in vitro