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VAF347 is an agonist of the aryl hydrocarbon receptor (AhR).1 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; Item No. 71820) and promotes differentiation of HL-60 cells induced by all-trans retinoic acid (Item No. 11017).2 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.3 VAF347 (30 mg/kg) also prevents retinal capillary degeneration in a mouse model of diabetic retinopathy induced by streptozotocin (STZ; Item No. 13104).4
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1. Activation of the aryl hydrocarbon receptor is essential for mediating the anti-
2. The AhR agonist VAF347 augments retinoic acid-
3. A novel low molecular weight inhibitor of dendritic cells and B cells blocks allergic inflammation. Am. J. Respir. Crit. Care Med. 173(6), 599-606 (2006).
4. Aryl hydrocarbon receptor agonist VAF347 impedes retinal pathogenesis in diabetic mice. Int. J. Mol. Sci. 22(9), 4335 (2021).