BAY-218 (AHR antagonist 1)
Catalog No.: GC35271Purity:>99.00%Synonyms: AHR antagonist 1
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.
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Cas No.: 2162982-11-6
10mM (in 1mL DMSO)In Stock
$76.00
1
5mgIn Stock
$70.00
1
10mgIn Stock
$121.00
1
25mgIn Stock
$269.00
1
50mgIn Stock
$454.00
1
100mgIn Stock
$788.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $76.00 | In Stock | 1 | |
| 5mg | $70.00 | In Stock | 1 | |
| 10mg | $121.00 | In Stock | 1 | |
| 25mg | $269.00 | In Stock | 1 | |
| 50mg | $454.00 | In Stock | 1 | |
| 100mg | $788.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
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].
Protocol
| 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: | |
Product Documents
Purity:>99.00%Appearance:A solid
Chemical Properties
CAS No.
2162982-11-6
Synonyms
AHR antagonist 1
SMILES
O=C(C1=CC(C2=CC=C(Cl)C=C2)=NN(C3=CC=CC(F)=C3)C1=O)N[C@@H](C)CO
Molecular Formula
C20H17ClFN3O3
Molecular Weight
401.82
Solubility
DMSO: ≥ 250 mg/mL (622.17 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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