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      AMG 837 (sodium salt)研究進(jìn)展

      發(fā)布日期:2017-11-02   瀏覽次數(shù):0
      核心提示:a href=https://www.medchemexpress.com/AMG-837-sodium-salt.htmlAMG 837 (sodium salt)/a產(chǎn)品描述:AMG 837 sodium salt is a
      AMG 837 (sodium salt)產(chǎn)品描述:AMG 837 sodium salt 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 pote


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      產(chǎn)品鏈接:www.medchemexpress.cn/amg-837-sodium-salt.html

       
       
       
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