| Identification | Back Directory | [Name]
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)- | [CAS]
2421141-40-2 | [Synonyms]
GLUT inhibitor-1
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)- | [Molecular Formula]
C32H35N7O2 | [MOL File]
2421141-40-2.mol | [Molecular Weight]
549.67 |
| Chemical Properties | Back Directory | [Boiling point ]
752.1±60.0 °C(Predicted) | [density ]
1.36±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
14.10±0.50(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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. | [in vivo]
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) | 2525 | 1675 | | oral AUC (ng/mL) | 5890 | 6813 | | CL (mL/min/kg) | 40 | 37 | | Vdss (L/Kg) | 1.70 | 4.51 | | t1/2 (h) | 0.785 | 2.59 | | F (%) | 45.4 | 49.4 | | B/Pb | 0.05 | |
b: Solubility is determined in PBS buffer solutions.
| [IC 50]
GLUT1: 242 nM (IC50); GLUT3: 179 nM (IC50) | [References]
[1]. Liu KG, et al. Discovery and Optimization of Glucose Uptake Inhibitors. J Med Chem. 2020;63(10):5201-5211. |
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