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编 号：F215419
分子式：C23H31NO4S
分子量：417.56
分子式：C23H31NO4S
分子量：417.56
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CAS No: 178961-24-5
产品详情
生物活性：
264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action.
体内研究：
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. 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.
体外研究：
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.
264W94 is a potent ileal bile acid transporter (IBAT) inhibitor and a new cholesterol lowering agent. 264W94 has CYP7A1 induction, and antilipemic action.
体内研究：
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. 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.
体外研究：
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.
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