264W 94
| 中文名称 | 264W 94 |
|---|---|
| 中文同义词 | 化合物 T10090 |
| 英文名称 | 264W 94 |
| 英文同义词 | 264W 94;264W94,264W-94;1,4-Benzothiazepine, 3-butyl-3-ethyl-2,3,4,5-tetrahydro-7,8-dimethoxy-5-phenyl-, 1,1-dioxide, (3R,5R)-rel- |
| CAS号 | 178961-24-5 |
| 分子式 | C23H31NO4S |
| 分子量 | 417.56 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 178961-24-5.mol |
| 结构式 |  |
264W 94 性质
| 沸点 | 553.0±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.112±0.06 g/cm3(Predicted) |
| 酸度系数(pKa) | 5.81±0.60(Predicted) |
IBAT
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 (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. |