GSK 137647
(Synonyms: 4-甲氧基-N-(2,4,6-三甲基苯)苯磺酰胺,GSK 137647) 目录号 : GC16176
A selective GPR120 agonist
Cas No.:349085-82-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Target: FFA4/GPR120
IC50: N/A
GSK137647A is potent and selective FFA4/GPR120 agonist with pEC50 values of 6.3, 6.2, and 6.1 at the human, mouse and rat receptor, respectively [1]. The free fatty acid receptor 4 (FFA4/GPR120), a member of the G protein-coupled receptor family, is a potential 7TM receptor involved in long-chain fatty acid-stimulated glucagon-like peptide-1 (GLP-1) secretion. FFA4 is highly expressed in the intestinal endocrine cell line STC-1 and the intestine [1]. GLP-1 regulates multiple physiological functions including eating behavior [2].
In vitro: GSK137647A (50 μM) induced a concentration-dependent increase in glucose (25 mM)-stimulated insulin secretion in MIN6 mouse insulinoma cell line [1]. In addition, GSK137647A (100 μM) induced a modest increase in GLP-1 secretion in the human intestinal cell line NCI-H716. Moreover, GSK137647A induced intracellular calcium accumulation in U2OS cells [1].
In vivo: GSK137647A (50 μM) induced active GLP-1 release by mouse circumvallate papillae (CVPs) [2].
References:
1. Sparks SM, Chen G, Collins JL, Danger D, Dock ST, Jayawickreme C, et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014;24(14):3100-3.
2. Martin C, Passilly-Degrace P, Chevrot M, Ancel D, Sparks SM, Drucker DJ, et al. Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity. J Lipid Res. 2012;53(11):2256-65.
| Cas No. | 349085-82-1 | SDF | |
| 别名 | 4-甲氧基-N-(2,4,6-三甲基苯)苯磺酰胺,GSK 137647 | ||
| 化学名 | N-mesityl-4-methoxybenzenesulfonamide | ||
| Canonical SMILES | CC1=CC(C)=C(NS(C2=CC=C(OC)C=C2)(=O)=O)C(C)=C1 | ||
| 分子式 | C16H19NO3S | 分子量 | 305.39 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS(pH 7.2) (1:2): 0.25 mg/ml,Ethanol: 1 mg/ml | 储存条件 | Store at RT |
| 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 | 3.2745 mL | 16.3725 mL | 32.745 mL |
| 5 mM | 0.6549 mL | 3.2745 mL | 6.549 mL |
| 10 mM | 0.3275 mL | 1.6373 mL | 3.2745 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。