| AG-041Rgastrin/cholecystokinin-2 (CCKB) receptor antagonist |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
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Chemical structure
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| Cas No. | 159883-95-1 | SDF | Download SDF |
| Chemical Name | (3R)-1-(2,2-diethoxyethyl)-2,3-dihydro-N-(4-methylphenyl)-3-[[[(4-methylphenyl)amino]carbonyl]amino]-2-oxo-1H-indole-3-acetamide | ||
| Canonical SMILES | CC1=CC=C(NC(N[C@@]2(C3=C(C=CC=C3)N(CC(OCC)OCC)C2=O)CC(NC4=CC=C(C)C=C4)=O)=O)C=C1 | ||
| Formula | C31H36N4O5 | M.Wt | 544.7 |
| 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 [1]. 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 [2].
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 [1]. In chondrocytes incubated with 0.1 and 1 μM AG-041R, synthesis of GAG increased with culture, and amounts accumulated in the composites increased [1]. 10 μM AG-041R might be even toxic to the cells and total RNA levels [1]. 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 [1].
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 [1].
References:[1] 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.[2] 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.
