A nonpeptide CCK receptor antagonist; selectively binds to CCK1 receptors in rat pancreas (IC50 = 0.58 nM) over CCK2 receptors in guinea pig cortex and gastrin receptors in guinea pig gastric glands (IC50s = 489 and 2

SR 27897 – 50 mg

Brand:
Cayman
CAS:
136381-85-6
Storage:
-20
UN-No:
Non-Hazardous - /

SR 27897 is a nonpeptide cholecystokinin (CCK) receptor antagonist.{42981} It selectively binds to CCK1 receptors in rat pancreatic membranes (IC50 = 0.58 nM) over CCK2 receptors in guinea pig cortical membranes and gastrin receptors in guinea pig gastric gland suspensions (IC50s = 489 and 2,883 nM, respectively). SR 27897 inhibits amylase secretion induced by CCK in isolated rat pancreatic acini (pA2 = 7.50) and CCK-induced guinea pig gallbladder contractions ex vivo (pA2 = 9.57). It completely reverses CCK-induced amylase secretion in rats when administered at a dose of 1 mg/kg. SR 27897 also inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 μg/kg, respectively). SR 27897 inhibits gallbladder emptying in a mouse model of egg yolk-stimulated endogenous CCK release (ED50 = 27 μg/kg).  

 

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Description

A nonpeptide CCK receptor antagonist; selectively binds to CCK1 receptors in rat pancreas (IC50 = 0.58 nM) over CCK2 receptors in guinea pig cortex and gastrin receptors in guinea pig gastric glands (IC50s = 489 and 2,883 nM, respectively); inhibits CCK-induced amylase secretion in isolated rat pancreatic acini (pA2 = 7.50); inhibits CCK-induced guinea pig gallbladder contractions (pA2 = 9.57); completely reverses CCK-induced amylase secretion in rats at 1 mg/kg; inhibits CCK-induced gastric and gallbladder emptying in mice (ED50s = 3 and 72 μg/kg, respectively); inhibits gallbladder emptying in a mouse model of egg yolk-stimulated endogenous CCK release (ED50 = 27 μg/kg)

Formal name: 2-[[[4-(2-chlorophenyl)-2-thiazolyl]amino]carbonyl]-1H-indole-1-acetic acid

Synonyms:  Lintitript

Molecular weight: 411.9

CAS: 136381-85-6

Purity: ≥98%

Formulation: A solid

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