IBAT

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 75 SeHCAT in a dose-dependent manner. 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. 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 Result: Dose-dependently attenuated diet-induced increases in serum LDL+VLDL-C, as well as the decrease in HDL-C.

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 with IC 50 of 0.25 μM in CHO-hIBAT cells.

264W94 是有效的回肠胆汁酸转运蛋白 (IBAT) 抑制剂，是新型降胆固醇药。264W94 具有 CYP7A1 诱导作用和抗血脂作用。