BAY-218 (AHR antagonist 1)
Catalog No.: GC35271Purity:>99.00%Synonyms: AHR antagonist 1
مناهض AHR 1 (مناهض AHR 1) هو مضاد لمستقبلات هيدروكربون أريل (AHR).
المنتجات مخصصة للاستخدام البحثي فقط، وليست للاستخدام البشري. نحن لا نبيع للمرضى.
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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المراجع (Citations)
1 publicationsمنشورات الباحثين الذين استخدموا هذا المنتجالوصف (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].
البروتوكول (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: | |
وثائق المنتج (Product Documents)
Purity:>99.00%Appearance:A solid
الخصائص الكيميائية (Chemical Properties)
رقم CAS
2162982-11-6
المرادفات
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
الصيغة الجزيئية
C20H17ClFN3O3
الوزن الجزيئي
401.82
الذوبانية
DMSO: ≥ 250 mg/mL (622.17 mM)
التخزين
Store at -20°C
إرشادات عامة
اختر مذيبًا مناسبًا وفقًا لبيانات ذوبانية المنتج. بعد التحضير، قسّم المحلول المخزون إلى أجزاء لتجنب دورات التجميد والذوبان المتكررة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
استخدم المحاليل المخزونة خلال 6 أشهر عند حفظها في -80°C، أو خلال شهر واحد عند حفظها في -20°C.
لتحسين الذوبانية، سخّن الأنبوب إلى 37°C وعرّضه للموجات فوق الصوتية لمدة مناسبة.
شروط الشحن
تُشحن عينات التقييم مع عبوات تبريد. وتُشحن الأحجام الأخرى المتاحة في درجة حرارة الغرفة، أو مع عبوات تبريد عند الطلب.
الحاسبات (Calculators)المولارية / التخفيف / الوزن الجزيئي / تحويل الوحدات / تركيبة داخل الجسم الحي / الذوبانية
g/mol
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