169042-78-8
Chemical Structure
T-0632
- CAS. Nr.: 169042-78-8
- Formula:C28H21FN3NaO5
- Molecular Weight:521.47
IUPAC Name: (S)-3-(1-(2-fluorophenyl)-3-(isoquinoline-3-carboxamido)-6-methoxy-2-oxoindolin-3-yl)propanoic acid, sodium salt
InChIKey: DPPSUKHKHUMCCO-JCOPYZAKSA-N
SMILES: 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
Biological Activity: 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.
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T-0632 | 99.88% | 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. | ||||||||||||||||||||
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