Home Metabolism AhR inhibitor BAY-218 For research use only.

BAY-218

Synonyms: AHR antagonist 1

BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands.

BAY-218 Chemical Structure

BAY-218 Chemical Structure

CAS No. 2162982-11-6

Purity & Quality Control

Batch: S884201 DMSO]80 mg/mL]false]Ethanol]20 mg/mL]false]Water]Insoluble]false Purity: 99.96%
99.96

BAY-218 Related Products

Biological Activity

Description BAY-218 is a potent and selective small-molecule AhR inhibitor, inhibiting AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands.
Targets
AhR [1]
In vitro
In vitro

Mechanistically, BAY-218 inhibits AhR nuclear translocation, dioxin response element (DRE)-luciferase reporter expression and AhR-regulated target gene expression induced by both exogenous and endogenous AhR ligands. In vitro, BAY-218 rescues TNFα production from kynurenic acid(KA)-suppressed LPS-treated primary human monocytes[1].
In Vivo
In vivo

In vivo, BAY-218 enhances anti-tumoral immune responses and reduced tumor growth in the syngeneic mouse tumor models CT26 and B16-OVA. Furthermore, BAY-218 enhances therapeutic efficacy of an anti-PD-L1 antibody in the CT26 model[1].

Chemical Information & Solubility

Molecular Weight 401.82 Formula

C20H17ClFN3O3
CAS No. 2162982-11-6 SDF --
Smiles CC(CO)NC(=O)C1=CC(=NN(C1=O)C2=CC(=CC=C2)F)C3=CC=C(C=C3)Cl
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 80 mg/mL ( (199.09 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
Batch:

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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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