264W94

264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action[1].

Signaling Pathways >> Others >> Others

IBAT[1]

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 IC50 of 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[1]. 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)[1] 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.

[1]. Root C, et al. Ileal bile acid transporter inhibition, CYP7A1 induction, and antilipemic action of 264W94. J Lipid Res. 2002 Aug;43(8):1320-30.

[2]. Chen L, et al. Inhibition of apical sodium-dependent bile acid transporter as a novel treatment for diabetes. Am J Physiol Endocrinol Metab. 2012 Jan 1;302(1):E68-76.