关附甲素
关附甲素 性质
| 沸点 | 541.5±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.43±0.1 g/cm3(Predicted) |
| 储存条件 | 4°C, away from moisture and light |
| 酸度系数(pKa) | 12.97±0.70(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
关附甲素 用途与合成方法
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.
关附甲素 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | HY-N1483 | 关附甲素 | 1394-48-5 | 1 mg | 1200 |
| 2024-11-08 | HY-N1483 | 关附甲素 | 1394-48-5 | 5 mg | 3500 |
