2. Immunology/Inflammation
  3. Aryl Hydrocarbon Receptor
  4. BAY-218

BAY-218  (Synonyms: AHR antagonist 1)

Cat. No.: HY-111449 Purity: 99.95%
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BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses.

For research use only. We do not sell to patients.

BAY-218 Chemical Structure

BAY-218 Chemical Structure

CAS No. : 2162982-11-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 121 In-stock
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10 mM * 1 mL in DMSO USD 121 In-stock
Solid
5 mg USD 110 In-stock
10 mg USD 165 In-stock
25 mg USD 319 In-stock
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Based on 1 publication(s) in Google Scholar

BAY-218 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

BAY-218 (AHR antagonist 1) is an aryl hydrocarbon receptor (AHR) antagonist. BAY-218 has AHR inhibitory activity with an IC50 of 39.9 nM in in U87 glioblastoma cells. BAY-218 can be used for the research of cancer or conditions with dysregulated immune responses[1].

IC50 & Target

IC50: 39.9 nM (AHR in human cell line)[1]
In Vitro

BAY-218 (example 23) (72 pM-20 μM) has AHR inhibitory activity with an IC50 of 39.9 μM in in U87 glioblastoma cells[1].
? BAY-218 (1 nM-3 μM) has CYP1A1 inhibitory activity with an IC50 of 70.7 μM in human monocytic U937 cell line[1].
? BAY-218 (1 μM) reverses KA-induced inhibition of TNFα production by LPS stimulated human monocytes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BAY-218 Related Antibodies

RT-PCR[1]

Cell Line: human monocytic U937 cells
Concentration: 1 nM-3 μM
Incubation Time:
Result: Regulated antagonise ligand-induced AHR gene in a dose-dependent manner.
In Vivo

BAY-218 (example 23) (p.o; 30 mg/kg; bid) has good anti-tumor effect combinated with aPD-L1[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c mice (subcutaneously CT26 cells)[1]
Dosage: 30 mg/kg
Administration: p.o, bid
Result: Significantly decreased tumors size combinated with aPD-L1.
Molecular Weight

401.82

Formula

C20H17ClFN3O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=CC(C2=CC=C(Cl)C=C2)=NN(C3=CC=CC(F)=C3)C1=O)N[C@@H](C)CO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (622.17 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4887 mL 12.4434 mL 24.8868 mL
5 mM 0.4977 mL 2.4887 mL 4.9774 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.18 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4887 mL 12.4434 mL 24.8868 mL 62.2169 mL
5 mM 0.4977 mL 2.4887 mL 4.9774 mL 12.4434 mL
10 mM 0.2489 mL 1.2443 mL 2.4887 mL 6.2217 mL
15 mM 0.1659 mL 0.8296 mL 1.6591 mL 4.1478 mL
20 mM 0.1244 mL 0.6222 mL 1.2443 mL 3.1108 mL
25 mM 0.0995 mL 0.4977 mL 0.9955 mL 2.4887 mL
30 mM 0.0830 mL 0.4148 mL 0.8296 mL 2.0739 mL
40 mM 0.0622 mL 0.3111 mL 0.6222 mL 1.5554 mL
50 mM 0.0498 mL 0.2489 mL 0.4977 mL 1.2443 mL
60 mM 0.0415 mL 0.2074 mL 0.4148 mL 1.0369 mL
80 mM 0.0311 mL 0.1555 mL 0.3111 mL 0.7777 mL
100 mM 0.0249 mL 0.1244 mL 0.2489 mL 0.6222 mL
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BAY-218 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAY-2182162982-11-6AHR antagonist 1BAY218BAY 218AHR antagonist1AHR antagonist-1Aryl Hydrocarbon ReceptorAhRaryl hydrocarbon receptor (AHR)U87 glioblastoma cellshuman monocytic U937 cellscancerimmuneInhibitorinhibitorinhibit

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