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BAY-876

Axon 2660
CAS:  1799753-84-6
Purity:  99%
  • Soluble in DMSO
  • MF:  C24H16F4N6O2
  • MW:  496.42

Description

BAY-876 is a highly potent, selective, and orally bioavailable GLUT1 inhibitor with an IC₅₀ value of 2 nM. In vitro pharmacokinetic (PK) data demonstrate excellent stability in liver microsomes and hepatocytes, while in vivo PK studies confirm high oral bioavailability and a long terminal half-life.

BAY-876 serves as a valuable tool for mechanistic studies of glucose transporters across biochemical, cellular and disease-model assays.

Key Features

  • Potent and orally bioavailable GLUT1 inhibitor (IC50 = 2 nM)
  • High Isoform Selectivity: Exhibits over 100-fold greater selectivity for GLUT1 than GLUT2, GLUT3, and GLUT4.
  • Glycolytic Metabolism Blocker: Reduces glucose uptake, ATP production, and lactate secretion.
  • Disulfidptosis Trigger: Induces metabolic cell death in SLC7A11 cancer cells.
  • Favorable Pharmacokinetics: Exhibits high cell permeability, low metabolic clearance in liver microsomes, and a long terminal half-life in vivo.

Applications

  • GLUT1 pharmacology and target-validation studies
  • GLUT1 pathway and signaling assays
  • Disease-relevant cellular and translational model systems
  • Transporter functional assays

More Information

Parent CAS No. 1799753-84-6
Chemical Name N4-(1-(4-Cyanobenzyl)-5-methyl-3-(trifluoromethyl)-1H-pyrazol-4-yl)-7-fluoroquinoline-2,4-dicarboxamide
SMILES C12C=CC(F)=CC=1N=C(C(N)=O)C=C2C(=O)NC1=C(C)N(CC2C=CC(C#N)=CC=2)N=C1C(F)(F)F
MFCD N.A.
InChi InChI=1S/C24H16F4N6O2/c1-12-20(21(24(26,27)28)33-34(12)11-14-4-2-13(10-29)3-5-14)32-23(36)17-9-19(22(30)35)31-18-8-15(25)6-7-16(17)18/h2-9H,11H2,1H3,(H2,30,35)(H,32,36)
InChiKey BKLJDIJJOOQUFG-UHFFFAOYSA-N
CID 118191391
Short Description GLUT1 inhibitor

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