Description
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 .
Product information
CAS Number: 159883-95-1
Molecular Weight: 544.64
Formula: C31H36N4O5
Chemical Name: 2-[(3R)-1-(2,2-diethoxyethyl)-3-{[(4-methylphenyl)carbamoyl]amino}-2-oxo-2,3-dihydro-1H-indol-3-yl]-N-(4-methylphenyl)acetamide
Smiles: CC1C=CC(=CC=1)NC(=O)C[C@@]1(NC(=O)NC2C=CC(C)=CC=2)C2C=CC=CC=2N(CC(OCC)OCC)C1=O
InChiKey: KOLPMNSDISYEBU-WJOKGBTCSA-N
InChi: InChI=1S/C31H36N4O5/c1-5-39-28(40-6-2)20-35-26-10-8-7-9-25(26)31(29(35)37,19-27(36)32-23-15-11-21(3)12-16-23)34-30(38)33-24-17-13-22(4)14-18-24/h7-18,28H,5-6,19-20H2,1-4H3,(H,32,36)(H2,33,34,38)/t31-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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