| Description | TUG-424 significantly enhances glucose-stimulated insulin secretion at 100 nM. TUG-424 is a potent and selective free fatty acid receptor 1 agonist (EC50: 32 nM). |
| In vitro | 在相同葡萄糖浓度下,TUG-424 在12 mM 葡萄糖存在时对分泌的刺激作用约为2倍,与棕榈酸引起的刺激作用相当。TUG-424 的浓度增加(100 nM至10 µM)显著增强了葡萄糖刺激下的胰岛素分泌,100 nM时已显著,3 µM时效果最好。在2.8 mM 葡萄糖条件下,TUG-424 轻微但显著地减少了基础胰岛素分泌[1]。 |
| Target activity | FFA1/GPR40:(EC50)32 nM |
| Synonyms | TUG424 |
| molecular weight | 264.32 |
| Molecular formula | C18H16O2 |
| CAS | 1082058-99-8 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (189.16 mM) |
| References | 1. Discovery of Potent and Selective Agonists for the Free Fatty Acid Receptor 1 (FFA1/GPR40), a Potential Target for the Treatment of Type II Diabetes J. Med. Chem., 2008, 51 (22), pp 7061-7064 2. Christiansen E, et al. 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. J Med Chem. 2008 Nov 27;51(22):7061-4. |