GLUT inhibitor-1

Names

[ Name ]:
GLUT inhibitor-1

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer

Research Areas >> Inflammation/Immunology

[Target]

GLUT1:242 nM (IC50)

GLUT3:179 nM (IC50)

[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.

[References]

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

Chemical & Physical Properties

[ Molecular Formula ]:
C₃₂H₃₅N₇O₂

[ Molecular Weight ]:
549.67

GLUT inhibitor-1

Names

Biological Activity

Chemical & Physical Properties

Related Compounds