GW9508
目录号 : GC12401
An agonist of GPR40
Cas No.:885101-89-3
Sample solution is provided at 25 µL, 10mM.
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GW9508 is a selective agonist of GPR40 and 120 with pEC50 value of 7.32 ± 0.03 and 5.46 ± 0.09, respectively [1].
GPR40/120 belongs to G protein-coupled receptors (GPCRs) family and is activated by free fatty acids. Mucosal inflammation induced the overexpression of GPR40, GPR120, and several inflammatory cytokines, with correlations between ileal concentrations of tumor necrosis factor (TNF)-α and GPR expression levels [2] [3].
GW9508 is a GPR40/120 agonist and is different from the reported GPR40/120 agonist GW1100. When tested with HEK-293 (human embryonic kidney) cells expressing GPR40 or GRP120, GW9508 treatment increased intracellular Ca2+ concentration via activating GPR40/120 in a dose-dependent manner [1]. In rat pancreaticβ-cells, GW9508 treatment activated KATP channels which inhibited GSIS through agonist of GPR40 and GPR120 [4]. When tested with TNF-α treated rat L cells, administration of GW9508 increased the expression of GLP-2 via activating GPR40 and 120 [2].
References:
[1].Briscoe, C.P., et al., Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol, 2006. 148(5): p. 619-28.
[2].Tsukahara, T., et al., Tumor necrosis factor alpha decreases glucagon-like peptide-2 expression by up-regulating G-protein-coupled receptor 120 in Crohn disease. Am J Pathol, 2015. 185(1): p. 185-96.
[3].Habib, A.M., et al., Co-localisation and secretion of glucagon-like peptide 1 and peptide YY from primary cultured human L cells. Diabetologia, 2013. 56(6): p. 1413-6.
[4].Zhao, Y.F., et al., GW9508 inhibits insulin secretion by activating ATP-sensitive potassium channels in rat pancreatic beta-cells. J Mol Endocrinol, 2013. 51(1): p. 69-77.
| Cas No. | 885101-89-3 | SDF | |
| 化学名 | 3-[4-[(3-phenoxyphenyl)methylamino]phenyl]propanoic acid | ||
| Canonical SMILES | C1=CC=C(C=C1)OC2=CC=CC(=C2)CNC3=CC=C(C=C3)CCC(=O)O | ||
| 分子式 | C22H21NO3 | 分子量 | 347.41 |
| 溶解度 | ≥ 16.05mg/mL in DMSO | 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 | 2.8784 mL | 14.3922 mL | 28.7844 mL |
| 5 mM | 0.5757 mL | 2.8784 mL | 5.7569 mL |
| 10 mM | 0.2878 mL | 1.4392 mL | 2.8784 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