[(1S,3S,5R,8S,9R,10R,11R,14R,16S,17R,18S,19S)-10,19-diacetyloxy-9-hydroxy-5-methyl-12-methylidene-7-azaheptacyclo[9.6.2.01,8.05,17.07,16.09,14.014,18]nonadecan-3-yl] acetate | 78969-72-9

• 物质功能分类: 天然产物 - 生物碱
• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 异戊烯醇脂质
• 英文名称: [(1S,3S,5R,8S,9R,10R,11R,14R,16S,17R,18S,19S)-10,19-diacetyloxy-9-hydroxy-5-methyl-12-methylidene-7-azaheptacyclo[9.6.2.01,8.05,17.07,16.09,14.014,18]nonadecan-3-yl] acetate
• CAS: 78969-72-9
• 化学式: C₂₆H₃₃NO₇
• 分子量: 471.5
• InChiKey: CXQAPRGJWIADOG-HWBHJWRYSA-N

物化性质

• 沸点：
  551.0±50.0 °C(Predicted)
• 密度：
  1.39±0.1 g/cm3(Predicted)

制备方法与用途

生物活性

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。

靶点

IC50: 17.9 μM (HERG channel)

体外研究

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.

体内研究

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.

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）。