Loxiglumide

Loxiglumide

CAT N°: 25534
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From 83.00 70.55

Loxiglumide is a cholecystokinin (CCK) receptor antagonist that inhibits CCK-8 binding to central and peripheral CCK receptors with Ki values of 9.1 and 0.33 ?M, respectively.{41979} It inhibits CCK-8-induced release of acetylcholine from isolated guinea pig gallbladder (IC50 = 10 nM).{41980} Loxiglumide (50 ?M) reduces the invasion of PANC-1 and MiaPaCa-2 human pancreatic cancer cells by 83.1 and 82.9%, respectively, in vitro.{41981} Loxiglumide (10-5,000 ?M) reduces DNA synthesis in PC-TI and PC-YY human pancreatic cancer cells in a concentration-dependent manner (IC50s = 160 and 74 ?M, respectively).{41982} It reduces the tumor growth rate by 37.5 and 38%, respectively, in PC-TI and PC-YY mouse xenograft models when administered at a dose of 250 mg/kg. Loxiglumide is toxic to mice with LD50 values ranging from 440 to 500 mg/kg dependent on the route of administration. In a rat model of acute pancreatitis, loxiglumide (50 mg/kg, s.c.) reduces serum concentrations of CCK, amylase, and lipase by greater than 60%, as well as tissue hemorrhaging and acinar cell necrosis.{41983}

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