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产地 | 中国 |
品牌 | Chemstan |
货号 | CS-N1483 |
用途 | 标准品 |
包装规格 | 1mg |
纯度 | 98.00%% |
CAS编号 | 1394-48-5 |
是否进口 | 否 |
Description | Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes[1] . Guanfu base A also inhibits HERG channel current[2] . |
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IC50 & Target | CYP2D6[1] ; HERG channel[2] |
In Vitro | 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[1] . MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
In Vivo | 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] . MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
Molecular Weight | 429.51 |
Formula | C??H??NO? |
CAS No. | 1394-48-5 |
SMILES | O[C@@]12C3[C@]45[C@@]([C@@H]6O)([H])C1(CC([C@@]6([H])[C@H]2OC(C)=O)=C)C[C@@]7([H])[C@]4([H])[C@@](C)(C[C@H](OC(C)=O)C5)C[N@]37 |
Shipping | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
References |
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