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AMG 837

产品编号 T14216 CAS 865231-46-5

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. Overall, AMG 837 was both highly potent and selective in vitro. 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 and is a highly potent stimulator of insulin secretion in MIN6 cells with an EC50 comparable to that seen in the aequorin Ca2+-flux assay. IC50 value: 13 nM (EC50) [1] Target: GPR40 agonist AMG 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). showed no 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.

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AMG 837, CAS 865231-46-5

规格	价格/CNY	货期
1 mg	￥ 647	35日内发货
5 mg	￥ 1,980	35日内发货
10 mg	￥ 3,720	35日内发货
25 mg	￥ 8,480	35日内发货

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AMG 837 的其他形式现货产品:

AMG 837 calcium hydrate

其他形式的 AMG 837:

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生物活性

化学信息

存储 & 溶解度

参考文献

产品描述

AMG 837 is a partial GPR40 agonist with an EC50 value of 13 nM, showcasing 85% of the maximal activity displayed by DHA in standard assay conditions, indicating its high potency and selectivity in vitro. This compound excels as a GPR40 agonist with a notable pharmacokinetic profile, effectively stimulating insulin secretion in a glucose-dependent manner in rodents and demonstrating potent insulin secretion stimulation in MIN6 cells, with efficacy comparable to that observed in aequorin Ca2+-flux assays. Moreover, AMG 837 exhibits a two-fold increase in potency compared to its racemic counterpart on GPR40, with demonstrated activity across rat and mouse GPR40 versions (EC50 = 23 and 13 nM, respectively). It lacks significant activity against PPARα, δ, and γ in cell-based assays, and an analysis against an external panel of 64 receptors revealed negligible activity, except for a weak inhibition (IC50 = 3 μM) on the a2-adrenergic receptor.

分子量	438.44
分子式	C26H21F3O3
CAS No.	865231-46-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

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.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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