VAF347

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

WARNING This product is not for human or veterinary use.

1. Lawrence, B.P., Denison, M.S., Novak, H., et al. Activation of the aryl hydrocarbon receptor is essential for mediating the anti-inflammatory effects of a novel low-molecular-weight compound. Int. J. Mol. Sci. 112(4), 1158-1165 (2008).

2. Ibabao, C.N., Bunaciu, R.P., Schaefer, D.M.W., et al. The AhR agonist VAF347 augments retinoic acid-induced differentiation in leukemia cells. FEBS Open Bio. 5, 308-318 (2015).

3. Ettmayer, P., Mayer, P., Kalthoff, F., et al. 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. Zapadka, T.E., Lindstrom, S.I., Batoki, J.C., et al. Aryl hydrocarbon receptor agonist VAF347 impedes retinal pathogenesis in diabetic mice. Int. J. Mol. Sci. 22(9), 4335 (2021).