关附庚素
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- CAS号:
- 78969-72-9
- 英文名:
- Guan-fu base G
- 英文别名:
- Guan-fu base G;Guan fu base G;(2α,11α,13R)-Hetisan-2,11,13,14-tetrol 2,11,13-triacetate;Hetisan-2,11,13,14-tetrol, 2,11,13-triacetate, (2α,11α,13R)-
- 中文名:
- 关附庚素
- 中文别名:
- CBNumber:
- CB02160926
- 分子式:
- C26H33NO7
- 分子量:
- 471.54
- MOL File:
- 78969-72-9.mol
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关附庚素化学性质
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沸点:
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551.0±50.0 °C(Predicted)
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密度:
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1.39±0.1 g/cm3(Predicted)
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酸度系数(pKa):
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12.77±0.70(Predicted)
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关附庚素性质、用途与生产工艺
Guanfu base G 是一种从 Aconitum coreanum 中分离的抗心律失常生物碱。Guanfu base G 以 IC50 值为 17.9 μM 来抑制 HERG 通道电流。
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.
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Animal Model:
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Rats
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Dosage:
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5 mg/kg
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Administration:
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Intravenous injection; for 5, 15, 30, 45, 60, 120, 240, 360, 480, 600, 720, 960 and 1200 minutes (Pharmacokinetic study)
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Result:
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The pharmacokinetic behavior was better in rats, the T
1/2
was 4.16 hours.
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化学性质
白色结晶，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于毛茛科植物黄花乌头的块根（关白附）。
关附庚素
上下游产品信息
上游原料
下游产品
78969-72-9, 关附庚素 相关搜索:
- 生物碱
- 78969-72-9
- Hetisan-2,11,13,14-tetrol, 2,11,13-triacetate, (2α,11α,13R)-
- Guan-fu base G
- Guan fu base G
- (2α,11α,13R)-Hetisan-2,11,13,14-tetrol 2,11,13-triacetate