Zaragozic Acid A is a squalene synthetase inhibitor and fungal metabolite containing a novel 4,6,7-trihydroxy-2,8-dioxobicyclo[3.2.1]octane-3,4,5-tricarboxylic acid core. Squalene synthase catalyzes the first committed step in cholesterol synthesis, mediating the reductive dimerization of farnesyl pyrophosphate to produce squalene. Zaragozic Acid A is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase (Ki = 78 pM in vitro). Zaragozic Acid A dose-dependently reduces cholesterol synthesis in HepG2 cells (IC50 = 6 μM) and inhibits hepatic cholesterol synthesis in mice (ED50 = 0.2 mg/kg).
Product Properties
pKa
pKₐ: 1.47 (Predicted)
Associated Targets
FNTATclin Protein farnesyltransferase/geranylgeranyltransferase type-1 subunit alpha 0 Activities
