关附庚素
| 中文名称 | 关附庚素 |
|---|---|
| 中文同义词 | |
| 英文名称 | Guan-fu base G |
| 英文同义词 | (2α,11α,13R)-Hetisan-2,11,13,14-tetrol 2,11,13-triacetate;Guan fu base G;Guan-fu base G;Hetisan-2,11,13,14-tetrol, 2,11,13-triacetate, (2α,11α,13R)- |
| CAS号 | 78969-72-9 |
| 分子式 | C26H33NO7 |
| 分子量 | 471.54 |
| EINECS号 | |
| 相关类别 | 生物碱 |
| Mol文件 | 78969-72-9.mol |
| 结构式 |  |
关附庚素 性质
| 沸点 | 551.0±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.39±0.1 g/cm3(Predicted) |
| 酸度系数(pKa) | 12.77±0.70(Predicted) |
IC50: 17.9 μM (HERG channel)
The effects of Guanfu base G is investigated in human embryonic kidney 293 (HEK293) cells transiently transfected with HERG complementary DNA using a whole-cell patch clamp technique. Guanfu base G inhibits HERG channel current in concentration-, voltage-, and time-dependent manners. Guanfu base G shifts the activation curve in a negative direction and accelerated channel inactivation but shows no effect on the inactivation curve. Moreover, Guanfu base G also accelerates channel recovery from inactivation.
Guanfu base G (5 mg/kg; intravenous injection; for 5-1200 minutes; rats) treatment in rats after 15 min could be detected the presence of Guanfu base A, about 10% of Guanfu base G in vivo could metabolize to Guanfu base A, which may be related to the metabolic enzymes in the body and its nature-related compounds, however, the substance in the body to eliminate more quickly, could be detected only around 240 min. The pharmacokinetic behavior of Guanfu base G is better in rats, the T 1/2 is 4.16 hours. These results indicate that Guanfu base G has a relatively suitable elimination half-life.
| Animal Model: | Rats |
| Dosage: | 5 mg/kg |
| Administration: | Intravenous injection; for 5, 15, 30, 45, 60, 120, 240, 360, 480, 600, 720, 960 and 1200 minutes (Pharmacokinetic study) |
| Result: | The pharmacokinetic behavior was better in rats, the T 1/2 was 4.16 hours. |