TUG-424 (CAS 1082058-99-8)
QUICK LINKS
TUG-424 is a potent and selective agonist of the free fatty acid receptor 1 (FFA1) or GPR40. Studies have demonstrated that TUG-424, at a concentration of 100nM, effectively enhances glucose-stimulated insulin secretion in INS-1E cells. FFA1 (GPR40) is predominantly expressed in pancreatic β-cells and is activated by medium and long-chain fatty acids. This receptor plays a role in amplifying glucose-stimulated insulin secretion. CAY10587 is another selective agonist of FFAR1 (GPR40), exhibiting an EC50 value of 32 nM. Notably, it does not affect other related receptors such as FFAR2 (GPR43) or FFAR3 (GPR41). CAY10587, at a concentration of 100 nM, effectively increases glucose-stimulated insulin secretion in INS-1E cells. TUG-424, acting as a potent and selective FFA1 agonist, holds promise in exploring the role of FFA1 in metabolic diseases. It has demonstrated the ability to enhance glucose-stimulated insulin secretion at a concentration of 100 nM in a rat beta-cell line and isolated mouse islets through FFA1 activation.
TUG-424 (CAS 1082058-99-8) References
- Discovery of potent and selective agonists for the free fatty acid receptor 1 (FFA(1)/GPR40), a potential target for the treatment of type II diabetes. | Christiansen, E., et al. 2008. J Med Chem. 51: 7061-4. PMID: 18947221
- Novel selective ligands for free fatty acid receptors GPR120 and GPR40. | Hara, T., et al. 2009. Naunyn Schmiedebergs Arch Pharmacol. 380: 247-55. PMID: 19471906
- Small molecules from natural sources, targeting signaling pathways in diabetes. | Liu, Q., et al. 2010. Biochim Biophys Acta. 1799: 854-65. PMID: 20601278
- A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents. | Luo, J., et al. 2012. PLoS One. 7: e46300. PMID: 23056280
- Discovery of a potent and selective free fatty acid receptor 1 agonist with low lipophilicity and high oral bioavailability. | Christiansen, E., et al. 2013. J Med Chem. 56: 982-92. PMID: 23294321
- Minireview: The effects of species ortholog and SNP variation on receptors for free fatty acids. | Hudson, BD., et al. 2013. Mol Endocrinol. 27: 1177-87. PMID: 23686113
- Mucus can change the permeation rank order of drug candidates. | Hagesaether, E., et al. 2013. Int J Pharm. 452: 276-82. PMID: 23707884
- Recent developments in the discovery of FFA1 receptor agonists as novel oral treatment for type 2 diabetes mellitus. | Defossa, E. and Wagner, M. 2014. Bioorg Med Chem Lett. 24: 2991-3000. PMID: 24881568
- Label-free biosensor assays in GPCR screening. | Grundmann, M. and Kostenis, E. 2015. Methods Mol Biol. 1272: 199-213. PMID: 25563186
- Activity of dietary fatty acids on FFA1 and FFA4 and characterisation of pinolenic acid as a dual FFA1/FFA4 agonist with potential effect against metabolic diseases. | Christiansen, E., et al. 2015. Br J Nutr. 113: 1677-88. PMID: 25916176
- GPR40 agonists for the treatment of type 2 diabetes mellitus: The biological characteristics and the chemical space. | Chen, C., et al. 2016. Bioorg Med Chem Lett. 26: 5603-5612. PMID: 27825762
- ω-3 Polyunsaturated fatty acids accelerate airway repair by activating FFA4 in club cells. | Lee, KP., et al. 2017. Am J Physiol Lung Cell Mol Physiol. 312: L835-L844. PMID: 28314803
- In Silico Searching for Alternative Lead Compounds to Treat Type 2 Diabetes through a QSAR and Molecular Dynamics Study. | Cabrera, N., et al. 2022. Pharmaceutics. 14: PMID: 35213965
Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
TUG-424, 5 mg | sc-222379 | 5 mg | $278.00 | |||
TUG-424, 25 mg | sc-222379A | 25 mg | $909.00 |