关附庚素
- CAS号:78969-72-9
- 英文名:Guan-fu base G
- 中文名:关附庚素
- CBNumber:CB02160926
- 分子式:C26H33NO7
- 分子量:471.54
- MOL File:78969-72-9.mol
- 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)
关附庚素性质、用途与生产工艺
- 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）。
- 公司名称：TargetMol Chemicals Inc.
- 联系电话：
- 电子邮件：support@targetmol.com
- 国家：美国
- 产品数：38631
- 优势度：58
- 公司名称：MedChemExpress
- 联系电话：--
- 电子邮件：sales@medchemexpress.com
- 国家：美国
- 产品数：6398
- 优势度：58
