BAY-218 (AHR antagonist 1)
Catalog No.: GC35271Purity:>99.00%Synonyms: AHR antagonist 1
AHR-Antagonist 1 (AHR-Antagonist 1) ist ein Aryl-Kohlenwasserstoff-Rezeptor (AHR)-Antagonist.
Die Produkte sind ausschließlich für Forschungszwecke bestimmt. Nicht zur Anwendung am Menschen. Wir verkaufen nicht an Patienten.
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 |
Tel: (909) 407-4943 / (909) 689-7124Email: sales@glpbio.com
Zitate (Citations)
1 publicationsPublikationen von Forschern, die dieses Produkt verwendenBeschreibung (Description)
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].
Protokoll (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: | |
Produktdokumente (Product Documents)
Purity:>99.00%Appearance:A solid
Chemische Eigenschaften (Chemical Properties)
CAS-Nr.
2162982-11-6
Synonyme
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
Summenformel
C20H17ClFN3O3
Molekulargewicht
401.82
Löslichkeit
DMSO: ≥ 250 mg/mL (622.17 mM)
Lagerung
Store at -20°C
Allgemeine Hinweise
Wählen Sie anhand der Löslichkeitsdaten des Produkts ein geeignetes Lösungsmittel. Aliquotieren Sie die Stammlösung nach der Herstellung, um wiederholte Gefrier-Auftau-Zyklen zu vermeiden.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Verwenden Sie Stammlösungen bei Lagerung bei -80°C innerhalb von 6 Monaten bzw. bei -20°C innerhalb von 1 Monat.
Zur Verbesserung der Löslichkeit das Röhrchen auf 37°C erwärmen und für eine angemessene Dauer beschallen.
Versandbedingungen
Evaluierungsmuster werden mit Kühlakkus versandt. Andere verfügbare Größen werden bei Raumtemperatur oder auf Anfrage mit Kühlakkus versandt.
Rechner (Calculators)Molarität / Verdünnung / Molekulargewicht / Einheitenumrechnung / In-vivo-Formulierung / Löslichkeit
g/mol
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