A CCK receptor antagonist (Kis = 9.1 and 0.33 μM for CCK-8 binding to central and peripheral CCK receptors

Loxiglumide – 50 mg

Brand:
Cayman
CAS:
107097-80-3
Storage:
-20
UN-No:
Non-Hazardous - /

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 μM, respectively.{41979} It inhibits CCK-8-induced release of acetylcholine from isolated guinea pig gallbladder (IC50 = 10 nM).{41980} Loxiglumide (50 μM) 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 μM) reduces DNA synthesis in PC-TI and PC-YY human pancreatic cancer cells in a concentration-dependent manner (IC50s = 160 and 74 μM, 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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Description

A CCK receptor antagonist (Kis = 9.1 and 0.33 μM for CCK-8 binding to central and peripheral CCK receptors, respectively); inhibits CCK-8-induced release of acetylcholine from isolated guinea pig gallbladders (IC50 = 10 nM); reduces the invasion of PANC-1 and MiaPaCa-2 human pancreatic cancer cells at 50 μM; reduces DNA synthesis in PC-TI and PC-YY human pancreatic cancer cells (IC50s = 160 and 74 μM, respectively); reduces tumor growth rate in PC-TI and PC-YY mouse xenograft models at 250 mg/kg; toxic to mice (LD50s = 440-500 mg/kg); reduces serum concentrations of CCK, amylase, and lipase as well as tissue hemorrhaging and acinar cell necrosis in a rat model of acute pancreatitis at 50 mg/kg

Formal name: 4-[(3,4-dichlorobenzoyl)amino]-5-[(3-methoxypropyl)pentylamino]-5-oxo-pentanoic acid

Synonyms:  CR1505

Molecular weight: 461.4

CAS: 107097-80-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Small Molecule Inhibitors|MMPs||Product Type|Biochemicals|Small Molecule Inhibitors|Nucleic Acid Turnover/Signaling||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|DNA Damage and Repair

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