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AMG 837 sodium salt
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AMG 837 sodium salt图片
CAS NO:865231-45-4
规格:98%
分子量:460.42
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议

产品介绍
AMG 837钠盐是GPR40激动剂,EC50为13 nM,具有较好的药代动力学表现。
CAS:865231-45-4
分子式:C26H20F3NaO3
分子量:460.42
纯度:98%
存储:Store at -20°C

Background:

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 potentand selective in vitro.




[1]. 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. [2]. Houze JB, et al. AMG 837: a potent, orally bioavailable GPR40 agonist. Bioorg Med Chem Lett. 2012 Jan 15;22(2):1267-70.