Guanfu base A
作者：齐岳
发布时间：2023-08-23
09:36:23
点击数：
产品名称：Guanfu base A
产品描述：
| 植物来源 | 天然产物 > 毛茛科 > 乌头属 |
| 结构类型 | 天然产物 > 生物碱 |
| 产品描述 | Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current. |
| 靶点活性 | CYP2D6:0.37 μM (Ki, cell free) |
| 体外活性 | Guanfu base A has no inhibitory activity on mouse or rat CYP2Ds. Guanfu base A does not exhibit any inhibition activity on human recombinant 2C8, 2C19, CYP1A2, 2A6, 3A4, or 3A5, but shows slight inhibition of 2B6 and 2E1. Guanfu base A is a potent inhibitor of CYP2D6, with an IC50 recorded at ~0.46 μM in HLM (Dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (Bufuralol 5 μM)[1]. Guanfu base A inhibits HERG channel current in concentration-, voltage-, and time-dependent manners with an IC50 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 [2]. |
| 体内活性 | Beagle dogs treated intravenously with Dextromethorphan (2 mg/mL) after pretreatment with Guanfu base A injection shows reduced CYP2D metabolic activity, with the Cmax 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 [1]. |
| 别名 | 关附甲素, Guan-fu base A |
| 分子量 | 429.513 |
| 分子式 | C24H31NO6 |
| CAS No. | 1394-48-5 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 10 mM
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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