AM-1638
目录号 : GC31607
AM-1638是有效，有口服活性的GPR40/FFA1激动剂，EC50值为0.16μM。
Cas No.:1142214-62-7
Sample solution is provided at 25 µL, 10mM.
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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.
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. | |
| Cas No. | 1142214-62-7 | SDF | |
| Canonical 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 |
| 溶解度 | DMSO: 250 mg/mL (485.79 mM) | 储存条件 | 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℃，然后在超声波浴中震荡一段时间。 |
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| 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。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9431 mL | 9.7157 mL | 19.4314 mL |
| 5 mM | 0.3886 mL | 1.9431 mL | 3.8863 mL |
| 10 mM | 0.1943 mL | 0.9716 mL | 1.9431 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet