Acetamide, 2-[3-[6-cyclobutyl-5,6,7,8-tetrahydro-4-[[4-(1H-pyrazol-4-yl)phenyl]amino]pyrido[4,3-d]pyrimidin-2-yl]phenoxy]-N-(1-methylcyclopropyl)-

GLUT inhibitor-1 is a potent and orally active inhibitor of glucose transporters, targeting both GLUT1 and GLUT3, with IC50s of 242 nM and 179 nM, respectively. GLUT inhibitor-1 has the potential for the reaesrch of cancers and autoimmune diseases[1]. Summary of the pharmacokinetic parameters of GLUT inhibitor-1 (compound 15b; 30 mg/kg) in mouse and rat[1]. Parameter Mouse Rat oral Cmax (ng/mL)25251675 oral AUC (ng/mL)58906813 CL (mL/min/kg)4037 Vdss (L/Kg)1.70 4.51 t1/2 (h)0.7852.59 F (%)45.449.4 B/Pb0.05b: Solubility is determined in PBS buffer solutions.

[1]. Liu KG, et al. Discovery and Optimization of Glucose Uptake Inhibitors. J Med Chem. 2020;63(10):5201-5211.