BAY-218 (AHR antagonist 1) (Synonyms: AHR antagonist 1) |
| Catalog No.GC35271 |
BAY-218 (AHR antagonist 1) is a novel, selective, and potent AhR small molecule inhibitor. 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.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2162982-11-6
Sample solution is provided at 25 µL, 10mM.
BAY-218 (AHR antagonist 1) is a novel, selective, and potent AhR small molecule inhibitor. 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[1].
In vitro, BAY-218 (0.1, 0.3 and 1μM; 18h) is able to reverse the inhibitory effect of kynurenic acid (KA) on the production of tumor necrosis factor alpha (TNFα) by lipopolysaccharide (LPS)-stimulated human primary monocytes[2].
In vivo, BAY-218 (30mg/kg; twice daily; p.o.) enhanced the therapeutic effect of anti-PD-L1 antibody in the CT26 mouse tumor model[2].
References:
[1] Gutcher I, Kober C, Roese L, et al. Abstract 1288: Blocking tumor-associated immune suppression with BAY-218, a novel, selective aryl hydrocarbon receptor (AhR) inhibitor[J].Experimental and Molecular Therapeutics, 2019.
[2] Schmees N, Gutcher I, Irlbacher H, et al. 3-oxo-2,6-diphenyl-2,3-dihydropyridazine-4-carboxamides: US201716303539[P]. US11040035B2[2025-10-07].
| Cell experiment [1]: | |
Cell lines | Human monocytes |
Preparation Method | Human monocytes were purified by negative selection using magnetic beads from donor PBMCs and seeded at a concentration of 2×10⁵ cells/well in complete growth medium (RPMI 1640, 10% fetal calf serum). Monocytes were incubated with 10ng/mL LPS and 200mM KA, and BAY-218 was added at concentrations of 1μM, 0.3μM, and 0.1μM, followed by culturing for 18h. LPS alone served as the positive control. TNFα production in the supernatant was measured using the Meso Scale Discovery immunoassay, and the ability of BAY-218 to rescue TNFα production was calculated based on LPS stimulation and KA-induced inhibition. |
Reaction Conditions | 0.1, 0.3 and 1μM; 18h |
Applications | BAY-218 is able to reverse the inhibitory effect of kynurenic acid (KA) on the production of tumor necrosis factor alpha (TNFα) by lipopolysaccharide (LPS)-stimulated human primary monocytes. |
| Animal experiment [1]: | |
Animal models | Female Balb/c mice |
Preparation Method | Female Balb/c mice at the age of 8 weeks were assigned to the study. CT26 cells were cultivated in RPMI 1640 containing 10% fetal calf serum and were passaged at least 3 times before inoculation. Female Balb/c mice were inoculated subcutaneously in the flank with 500,000 CT26 tumor cells (50% medium/50% matrigel). After 4 days, the animals were randomized, and treatment began on day 5. The BAY-218 at 30mg/kg was dissolved in ethanol/solutol/water (10/40/50) and administered orally twice daily, in combination with 10mg/kg of the anti-PD-L1 antibody administered intraperitoneally every 3 days. Tumor size was measured using calipers to determine length (a) and width (b). |
Dosage form | 30mg/kg; twice daily; p.o. |
Applications | BAY-218 enhanced the therapeutic effect of anti-PD-L1 antibody in the CT26 mouse tumor model. |
References: | |
| Cas No. | 2162982-11-6 | SDF | |
| Synonyms | AHR antagonist 1 | ||
| Canonical SMILES | O=C(C1=CC(C2=CC=C(Cl)C=C2)=NN(C3=CC=CC(F)=C3)C1=O)N[C@@H](C)CO | ||
| Formula | C20H17ClFN3O3 | M.Wt | 401.82 |
| Solubility | DMSO: ≥ 250 mg/mL (622.17 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4887 mL | 12.4434 mL | 24.8868 mL |
| 5 mM | 497.7 μL | 2.4887 mL | 4.9774 mL |
| 10 mM | 248.9 μL | 1.2443 mL | 2.4887 mL |
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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.
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Quality Control & SDS
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)
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