1394-48-5
1394-48-5 结构式
基本信息
关附甲素
关白附子甲素
关附甲素对照品
关附甲素标准品
盐酸关附甲素标准品
关附甲素,关白附子甲素
盐酸关附甲素,关白附子甲素
Guan-fu base A
Kwan-fu base A
Guan-fu base A USP/EP/BP
(2α,11α,13R)-Hetisan-2,11,13,14-tetrol 2,11-diacetate
Hetisan-2,11,13,14-tetrol,2,13-diacetate, (2a,11a,13R)-
Hetisan-2,11,13,14-tetrol, 2,13-diacetate, (2α,11α,13R)-
(2alpha,11alpha,13R)-Hetisan-2,11,13,14-tetrol 2,13-diacetate
物理化学性质
常见问题列表
CYP2D6; HERG channel
Guanfu base A has no inhibitory activity on mouse or rat CYP2Ds. Guanfu base A does not exhibit any inhibition activity on human recombinant CYP1A2, 2A6, 2C8, 2C19, 3A4, or 3A5, but shows slight inhibition of 2B6 and 2E1.
Guanfu base A is a potent inhibitor of CYP2D6, with an
IC
50
recorded at ~0.46 μM in HLM (Dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (Bufuralol 5 μM).
The effects of Guanfu base A is investigated in human embryonic kidney 293 (HEK293) cells transiently transfected with HERG complementary DNA using a whole-cell patch clamp technique. Guanfu base A inhibits HERG channel current in concentration-, voltage-, and time-dependent manners with an
IC
50
of 1.64 mM. Guanfu base A shifts the activation curve in a negative direction and accelerated channel inactivation but shows no effect on the inactivation curve.
Beagle dogs treated intravenously with Dextromethorphan (2 mg/mL) after pretreatment with Guanfu base A injection shows reduced CYP2D metabolic activity, with the C max of dextrorphan being one-third that of the saline-treated group and area under the plasma concentration-time curve half that of the saline-treated group.