AM-1638

目录号: GC31607纯度: >99.50%
AM-1638是有效,有口服活性的GPR40/FFA1激动剂,EC50值为0.16μM。

AM-1638
Cas No.: 1142214-62-7
规格价格库存数量操作
1mg¥1,227.00现货
1
5mg¥2,700.00现货
1
10mg¥4,320.00现货
1
10mM (in 1mL DMSO)¥3,057.00现货
1

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产品描述 Description

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.

实验参考方法 Experimental Reference Method

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].

References:

[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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1142214-62-7
SMILES
FC1=CC=C(OC)C=C1C2=C(C3=CCCC3(C)C)C=C(COC4=CC=CC([C@H](C5CC5)CC(O)=O)=C4)C=C2
分子式
C33H35FO4
分子量
514.63 g/mol
溶解性
DMSO: 250 mg/mL (485.79 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至 37°C,然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备 RT,或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol