1394-48-5
Chemical Structure
Guanfu base A
- CAS No.: 1394-48-5
- Formula:C24H31NO6
- Molecular Weight:429.51
IUPAC Name: (2S,3aR,3a1R,5S,5aS,7R,8R,9R,10S,10aS,10bS)-7,10-dihydroxy-3a-methyl-12-methylenedecahydro-1H,4H,7H-5,7,10b-(epimethanetriyl)-6a,9-ethanodibenzo[cd,f]indole-2,8-diyl diacetate
InChIKey: OGNUSOJAYIHLNS-DCOLOBNFSA-N
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
Biological Activity: 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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Guanfu base A | 98.10% | 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. Guanfu base A also inhibits HERG channel current. | ||||||||||||||||||||
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- [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. [Content Brief]
- [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. [Content Brief]
Keywords
