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| | AMG 837 Basic information |
| Product Name: | AMG 837 | | Synonyms: | AMG 837 calcium salt;AMG 837 hemicalcium salt;(βS)-β-1-Propyn-1-yl-4-[[4'-(trifluoromethyl)[1,1'-biphenyl]-3-yl]methoxy]benzenepropanoic acid hemicalcium salt;AMG 837 hemicalcium;(βS)-β-1-Propyn-1-yl-4-[[4'-(trifluoromethyl)[1,1'-biphenyl]-3-yl]methoxy]benzenepropanoicacidhemicalciumsalt | | CAS: | 1291087-14-3 | | MF: | C26H23CaF3O3 | | MW: | 480.54 | | EINECS: | | | Product Categories: | | | Mol File: | 1291087-14-3.mol |  |
| | AMG 837 Chemical Properties |
| storage temp. | Store at -20°C | | solubility | Soluble in DMSO |
| | AMG 837 Usage And Synthesis |
| Uses | AMG 837 Hemicalcium Salt is used in the synthetic preparation of a novel GPR40 receptor agonist, AMG 837 (A614410). GPR40 is a polyunsaturated fatty acid receptor that is involved with many systemic effects, which are beneficial for metabolic and inflammatory diseases. GPR40 has also been implicated as a target for treating obesity. | | in vivo | AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats[1].
AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo[1].
AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F=84%) and a total plasma Cmax of 1.4 μM[1]. | Animal Model: | 8-week old Zucker Fatty Rats[1] | | Dosage: | 0.03, 0.1, 0.3 mg/kg | | Administration: | Oral gavage once daily for 21 days | | Result: | Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively.
Increased insulin levels in the mid- and high-dose groups.
Not affected body weights during the 21-day treatment. |
| Animal Model: | 8-week old Sprague-Dawley rats[1] | | Dosage: | 0.03, 0.1, 0.3 mg/kg | | Administration: | A single p.o. administration | | Result: | Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg. |
| | storage | Store at +4°C |
| | AMG 837 Preparation Products And Raw materials |
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