Tebufenozide

Tebufenozide is an insecticide that acts as a non-steroidal agonist of the insect ecdysone receptor (EcR; IC₅₀ = 0.85 nM in a cell-free preparation of C. suppressalis integument).¹ It induces a premature molt and is lethal to S. litura third instar larva (LD₅₀ = 0.33 µM per larva).^1,2 It also inhibits P-glycoprotein (P-gp), also known as multidrug resistance protein 1 (MDR1), activity in LLC-PK1 porcine kidney epithelial cells expressing human P-gp (IC₅₀ = 21.5 µM).³ Tebufenozide has low toxicity in mammals, birds, and most aquatic species, but it dose-dependently decreases colony formation and induces apoptosis and cell cycle arrest in HeLa cells when used at concentrations ranging from 50 to 200 µg/ml.^4,5 Formulations containing tebufenozide have been used as insecticides, miticides, sex attractants, and/or feeding stimulants in agricultural, aquatic, and residential areas.

WARNING This product is not for human or veterinary use.

1. Minakuchi, C., Nakagawa, Y., Kamimura, M., et al. Binding affinity of nonsteroidal ecdysone agonists against the ecdysone receptor complex determines the strength of their molting hormonal activity. Eur. J. Biochem. 270(20), 4095-4104 (2003).

2. Yokoi, T., Minami, S., Nakagawa, Y., et al. Structure-activity relationship of imidazothiadiazole analogs for the binding to the ecdysone receptor of insect cells. Pestic. Biochem. Physiol. 120, 40-50 (2015).

3. Miyata, K.-i., Nakagawa, Y., Kimura, Y., et al. Structure-activity relationships of dibenzoylhydrazines for the inhibition of P-glycoprotein-mediated quinidine transport. Bioorg. Med. Chem. 24(14), 3184-3191 (2016).

4. Xu, W., Wang, B., Yang, M., et al. Tebufenozide induces G₁/S cell cycle arrest and apoptosis in human cells. Environ. Toxicol. Pharmacol. 49, 89-96 (2017).

5. Abass, K.M. An investigation into the formation of tebufenozide’s toxic aromatic amine metabolites in human in vitro hepatic microsomes. Pestic. Biochem. Physiol. 133, 73-78 (2016).