| Description | BAY-876 is an orally active and selective inhibitor of glucose transporter 1 (GLUT1, IC50= 2 nM). BAY-876 exhibits >130-fold more selective for GLUT1 than GLUT2, GLUT3, and GLUT4. BAY-876 also inhibits glycolytic metabolism and ovarian cancer growth. |
| In vitro | BAY-876 is a highly-selective GLUT1 inhibitor with selectivity over GLUT2, 3, and 4 of 4700-, 800-, and 135-fold, respectively[1]. |
| In vivo | BAY-876 displays low clearance also in?vivo in rat and in dog. The volume of distribution in steady state (Vss) is moderate in both species. Terminal half life is intermediate in rat (2.5 h) and long in dog (22 h) due to the very low clearance. The oral bioavailability (F%) is 85% and 79% in rat and dog, respectively. Preliminary in?vivo PK studies of BAY-876 demonstrate that a good oral bioavailability and long terminal half-life is attainable making it an excellent chemical probe to further evaluate the hypothesis of cancer treatment with a very selective GLUT1 inhibitor[1]. |
| Target activity | GLUT1:0.002 μM |
| molecular weight | 496.42 |
| Molecular formula | C24H16F4N6O2 |
| CAS | 1799753-84-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: 3 mg/mL (6.04 mM) DMSO: 15 mg/mL (30.23 mM), Sonication is recommended. |
| References | 1. Siebeneicher H, et al. ChemMedChem. 2016, 11(20):2261-2271. |
| Citations | 1. Pei Y, Lv S, Shi Y, et al. RAB21 controls autophagy and cellular energy homeostasis by regulating retromer-mediated recycling of SLC2A1/GLUT1. Autophagy. 2022: 1-17 2. Chen X, Zhao Y, He C, et al. Identification of a novel GLUT1 inhibitor with in vitro and in vivo anti-tumor activity. International Journal of Biological Macromolecules. 2022, 216: 768-778. 3. Zhang M, Tan Y, Song Y, et al.GLUT4 mediates the protective function of gastrodin against pressure overload-induced cardiac hypertrophy.Biomedicine & Pharmacotherapy.2023, 161: 114324. |