AMG 837
(Synonyms: (BETAS)-BETA-1-丙炔-1-基-4-[[4'-(三氟甲基)[1,1'-联苯]-3-基]甲氧基]苯丙酸) 目录号 : GC19030An FFAR1 (GPR40) partial
Cas No.:865231-46-5
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
AMG 837 is a potent GPR40 agonist(EC50=13 nM) with a superior pharmacokinetic profile and robust glucose-dependent stimulation of insulin secretion in rodents.IC50 value: 13 nM (EC50) [1]Target: GPR40 agonistAMG 837 displayed the expected two-fold increase in potency on GPR4 (EC50 = 13 [±7] nM) compared to the racemic compound and its activity crossed over to the rat and mouse forms of GPR40 (EC50 = 23 and 13 nM, respectively). AMG 837 was found to be a partial agonist on GPR40 with maximal activity 85% of that shown by DHA under our standard assay conditions. AMG 837 is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. showedno significant activity in cell-based assays against PPARα, δ, and γ. An external panel of 64 receptors also revealed no significant activity with the exception of weak inhibition (IC50 = 3 uM) on the a2-adrenergic receptor. Overall, AMG 837 was both highly potentand selective in vitro.
References:
[1]. Houze JB, et al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70.
[2]. Lin DC, et al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One. 2011;6(11):e27270.
Cas No. | 865231-46-5 | SDF | |
别名 | (BETAS)-BETA-1-丙炔-1-基-4-[[4'-(三氟甲基)[1,1'-联苯]-3-基]甲氧基]苯丙酸 | ||
Canonical SMILES | OC(C[C@H](C#CC)C1=CC=C(C=C1)OCC2=CC=CC(C3=CC=C(C(F)(F)F)C=C3)=C2)=O | ||
分子式 | C26H21F3O3 | 分子量 | 438.44 |
溶解度 | DMSO : ≥ 42 mg/mL (92.22 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.2808 mL | 11.4041 mL | 22.8081 mL |
5 mM | 0.4562 mL | 2.2808 mL | 4.5616 mL |
10 mM | 0.2281 mL | 1.1404 mL | 2.2808 mL |
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% DMSO % % Tween 80 % saline | ||||||||||
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2.
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