264W94 is a robust inhibitor of the ileal bile acid transporter (IBAT) and a novel agent for reducing cholesterol levels. It exhibits CYP7A1 induction and demonstrates significant antilipemic activity.

264W94 (0, 0.1, 0.25, 0.5 μM) inhibits human IBAT-specific transport of 5 μM TC by 14% to 75% in a concentration-dependent manner (IC50: 0.25 μM in CHO-hIBAT cells) [1].

264W94 (orally; 0.03-1.0 mg/kg; twice a day for 3.5 days) dose-dependently attenuates diet-induced increases in serum LDL+VLDL-C, as well as the decrease in HDL-C. 264W94 (orally; 0.003, 0.01, 0.03, 0.1 mg/kg; twice a day for 2 days) increases fecal excretion of 75SeHCAT in a dose-dependent manner [1]. 264W94 (0.001, 0.01, 0.1, 1, and 10 mg/kg; twice a day for 2 weeks) reduces dose-dependently plasma glucose in male ZDF (ZDF/GmiCrl-fa/fa) rats. Treatment of 264W94 prevents the decline of insulin dose-dependently without an increase in proinsulin levels [2].

Animal Model: Male Sprague Dawley rats (CD, Charles River, 270-310 gm). Dosage: 0.03, 0.1, 0.3, 1.0 mg/kg. Administration: Orally; twice a day (9:00 am and 3:30 pm) for 3.5 days [1]