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Guanfu base A
  • 品牌:Chemstan
  • 产地:中国
  • 货号:CS-N1483
  • cas:1394-48-5
  • 价格: ¥1000/支
  • 发布日期: 2020-11-30
  • 更新日期: 2025-09-22
产品详请
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
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] .

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] .
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] .
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 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] .

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
  • [1]. Sun J, et al. Guanfu base A, an antiarrhythmic alkaloid of Aconitum coreanum, Is a CYP2D6 inhibitor of human, monkey, and dog isoforms. Drug Metab Dispos. 2015 May;43(5):713-24.

    [2]. Huang X, et al. Comparative effects of Guanfu base A and Guanfu base G on HERG K+ channel. J Cardiovasc Pharmacol. 2012 Jan;59(1):77-83.


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