Бензарон

Химические свойства

Pale Yellow Solid

Всемирная организация здравоохранения(ВОЗ)

Benzarone is given by mouth and applied topically for treatment of various vascular peripheral disorders.The decision to suspend the marketing authorization results from several reports of toxic hepatitis, including one fatal case from within Germany. The product remains registered in Italy and France.

Биологическая активность

Benzarone is an active metabolite of the urate anion transporter 1 (URAT1) inhibitor benzbromarone. It inhibits URAT1 in Xenopus oocytes expressing the human enzyme (IC50 = 2.8 μM). Benzarone also inhibits the tyrosine phosphatase activity of eyes absent homolog 3 (EYA3; IC50 = 17.5 μM), as well as reduces the proliferation and migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 7.5 μM. It uncouples oxidative phosphorylation in isolated rat liver mitochondria and induces apoptosis and necrosis in isolated rat hepatocytes. Benzarone (25 μg/g) reduces tumor growth in an A-673 Ewing sarcoma mouse xenograft model.

Профиль безопасности

Poison by intraperitoneal route. An experimental teratogen. Other experimental reproductive effects. A flammable liquid. When heated to decomposition it emits acrid and irritating smoke and fumes. See also KETONES.