|AG-041R gastrin/cholecystokinin-2 (CCKB) receptor antagonist|
Sample solution is provided at 25 µL, 10mM.
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|Cas No.||159883-95-1||SDF||Download SDF|
|Canonical SMILES||CC1=CC=C(NC(N[[email protected]@]2(C3=C(C=CC=C3)N(CC(OCC)OCC)C2=O)CC(NC4=CC=C(C)C=C4)=O)=O)C=C1|
|Solubility||≤5mg/ml in DMSO;10mg/ml in dimethyl formamide||Storage||Store at -20°C|
|Physical Appearance||A crystalline solid||Shipping Condition||Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request|
|General tips||For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.|
AG-041R is a cholecystokinin-B/gastrin receptor (Gastrin/CCK-B) antagonist . The Gastrin/CCK-B receptor is a regulator of gastric acid secretion and mucosal growth. The Gastrin/CCK-B is abundantly expressed in mammalian stomach .
In vitro: In rabbit primary chondrocytes, AG-041R (0.1 μM) stimulated the cell growth and proliferation, but suppressed with 10 μM. Treatment with AG-041R (1 μM) for 28 days accelerated the chondrocyte growth and increased the cell number . In chondrocytes incubated with 0.1 and 1 μM AG-041R, synthesis of GAG increased with culture, and amounts accumulated in the composites increased . 10 μM AG-041R might be even toxic to the cells and total RNA levels . The ratio of the amounts of two chondroitin sulfate isomers, chondroitin-6-sulfate to chondroitin-4-sulfate, an indicator of cartilage maturation, increased with 1 μM but decreased with 10 μM AG-041R .
In vivo: In a preclinical toxicological study on rats, oral administration of high dose of AG-041R stimulated systemic cartilage hyperplasia, including the trachea, the intervertebral disk and the articular cartilage. Daily intraarticular injection of AG-041R for 3 weeks into rat knee joints also induced cartilage hyperplasia in marginal regions of the femoral condyle without affecting other tissues .
 Ochi M, Kawasaki K, Kataoka H, et al. AG-041R, a gastrin/CCK-B antagonist, stimulates chondrocyte proliferation and metabolism in vitro[J]. Biochemical and biophysical research communications, 2001, 283(5): 1118-1123.
 Langhans N, Rindi G, Chiu M, et al. Abnormal gastric histology and decreased acid production in cholecystokinin-B/gastrin receptor-deficient mice[J]. Gastroenterology, 1997, 112(1): 280-286.