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AM-1638
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。
AM-1638图片
规格:98%
分子量:514.63
包装与价格:
包装价格(元)
250mg电议
500mg电议

产品介绍
AM-1638是有效,有口服活性的GPR40/FFA1激动剂,EC50值为0.16μM。
货号:ajcx12624
CAS:1142214-62-7
分子式:C33H35FO4
分子量:514.63
溶解度:DMSO: 250 mg/mL (485.79 mM)
纯度:98%
存储:Store at -20°C
库存:现货

Background:

AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.


AM-1638 exhibits moderate cross-species plasma clearance and volume of distribution, resulting in plasma half-lives suitable for evaluation of its antidiabetic properties in mouse, rat, and cynomologus monkey. Moreover, oral administration of full agonist AM-1638 demonstrates excellent oral bioavailability (mouse, >100%; rat, 72%; and cyno, 71%). AM-1638exhibits antidiabetic activity in BDF/DIO mice[1].

[1]. Brown SP, et al. Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. ACS Med Chem Lett. 2012 Aug 15;3(9):726-30.

Protocol:

Animal experiment:

Mice[1]On the morning of the experiment, Male B6D2F1/J mice are fasted for four hours and body weight and blood glucose levels are measured. Animals are randomized into treatment groups based on these two parameters. Treatments are administered by oral gavage and sixty minutes later, the mice received a 2 g/kg glucose challenge dose by oral gavage (defined as t=0 min). Blood samples are collected at -60, 0, 15, 30, 60, 90 and 120 minutes via tail vein relative to the glucose challenge. Glucose levels are monitored with a glucometer. Plasma insulin is measured using a mouse insulin ELISA[1].

参考文献:

[1]. Brown SP, et al. Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. ACS Med Chem Lett. 2012 Aug 15;3(9):726-30.