VAF347

VAF347 is an agonist of the aryl hydrocarbon receptor (AhR). It binds to AhR in a radioligand binding assay using guinea pig hepatic cytosol and induces mRNA expression of the AhR target gene CYP1A1 in isolated human peripheral blood mononuclear cells (PBMCs) when used at a concentration of 50 nM. VAF347 (20 µM) inhibits differentiation of HL-60 leukemia cells induced by 1,25-dihydroxy vitamin D3 (calcitriol, Cay-71820) and promotes differentiation of HL-60 cells induced by all-trans retinoic acid (Cay-11017). It decreases serum IgE levels and lung and bronchoalveolar lavage fluid (BALF) eosinophil infiltration in an ovalbumin-induced mouse model of allergic inflammation when administered at a dose of 30 mg/kg. VAF347 (30 mg/kg) also prevents retinal capillary degeneration in a mouse model of diabetic retinopathy induced by streptozotocin (STZ, Cay-13104).Formal Name: 4-(3-chlorophenyl)-N-[4-(trifluoromethyl)phenyl]-2-pyrimidinamine. CAS Number: 574759-62-9. Molecular Formula: C17H11ClF3N3. Formula Weight: 349.7. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 5 mg/ml, DMSO: 1 mg/ml, Ethanol: Slightly soluble. lambdamax: 288 nm. SMILES: FC(F)(C1=CC=C(NC2=NC=CC(C3=CC(Cl)=CC=C3)=N2)C=C1)F. InChi Code: InChI=1S/C17H11ClF3N3/c18-13-3-1-2-11(10-13)15-8-9-22-16(24-15)23-14-6-4-12(5-7-14)17(19,20)21/h1-10H,(H,22,23,24). InChi Key: XTKUZTBZRIJTFR-UHFFFAOYSA-N.