| CAS NO: | 159883-95-1 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 159883-95-1 |
| 化学名 | (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 |
| 分子式 | C31H36N4O5 |
| 分子量 | 544.7 |
| 溶解度 | ≤5mg/ml in DMSO;10mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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