Home Metabolism GLUT inhibitor BAY-876 For research use only.

BAY-876

BAY-876 is a potent and selective GLUT1 inhibitor (IC50=0.002 μM) with a selectivity factor of >100 against GLUT2, GLUT3, and GLUT4.

BAY-876 Chemical Structure

BAY-876 Chemical Structure

CAS No. 1799753-84-6

Purity & Quality Control

BAY-876 Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hela-MaTu Function assay Cellular mechanistic assay: Inhibition of glucose uptake by Hela-MaTu cells, IC50 = 0.0032 μM. ChEMBL
Click to View More Cell Line Experimental Data

Biological Activity

Description BAY-876 is a potent and selective GLUT1 inhibitor (IC50=0.002 μM) with a selectivity factor of >100 against GLUT2, GLUT3, and GLUT4.
Targets
GLUT1 [1]
(Cell-free assay)
0.002 μM
In vitro
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].
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AMPK 30602670
Growth inhibition assay Cell viability 30602670
In Vivo
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].
Animal Research Animal Models Male Wistar rats
Dosages 0.3 mg/kg
Administration i.v.

Chemical Information & Solubility

Molecular Weight 496.42 Formula

C24H16F4N6O2
CAS No. 1799753-84-6 SDF --
Smiles CC1=C(C(=NN1CC2=CC=C(C=C2)C#N)C(F)(F)F)NC(=O)C3=CC(=NC4=C3C=CC(=C4)F)C(=O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 99 mg/mL ( (199.42 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

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% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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