GW9508 |
| Catalog No.GC12401 |
GW9508 est un agoniste puissant et sélectif des récepteurs couplés aux protéines G FFA1 (GPR40) et GPR120 avec des pEC50 de 7,32 et 5,46, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
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 | |
| Chemical Name | 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 | ||
| Formula | C22H21NO3 | M.Wt | 347.41 |
| Solubility | ≥ 16.05mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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