BAY-2416964

BAY-2416964 is an antagonist of the aryl hydrocarbon receptor (AhR, IC50 = 22 nM in U87 cells). It decreases the mRNA expression of the AhR target genes CYP1A1 and AHRR induced by the AhR agonist kynurenic acid (Cay-16792) in LPS-stimulated isolated human monocytes when used at a concentration of 100 nM. BAY-2416964 (30-1,000 nM) increases CD3-, CD28-, and IL-2-induced IFN-gamma production in isolated human naïve CD4+ T cells. In vivo, BAY-2416964 (30 mg/kg, p.o.) reduces tumor volume, increases CD8+ T cell and natural killer (NK) cell tumor infiltration, and decreases GR1+ myeloid cell and CD206+ M2 macrophage tumor infiltration in a B16/F10-OVA murine melanoma model.Formal Name: 6-(4-chlorophenyl)-2,3-dihydro-N-[(1S)-2-hydroxy-1-methylethyl]-2-(1-methyl-1H-pyrazol-4-yl)-3-oxo-4-pyridazinecarboxamide. CAS Number: 2242464-44-2. Molecular Formula: C18H18ClN5O3. Formula Weight: 387.8. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble: >10 mg/ml, Ethanol: Slightly soluble: 0.1-1 mg/ml. SMILES: O=C1N(C2=CN(C)N=C2)N=C(C3=CC=C(C=C3)Cl)C=C1C(N[C@@H](C)CO)=O. InChi Code: InChI=1S/C18H18ClN5O3/c1-11(10-25)21-17(26)15-7-16(12-3-5-13(19)6-4-12)22-24(18(15)27)14-8-20-23(2)9-14/h3-9,11,25H,10H2,1-2H3,(H,21,26)/t11-/m0/s1. InChi Key: YAGSZKAJPHGVOV-NSHDSACASA-N.