| Identification | Back Directory | [Name]
Guan-fu base A | [CAS]
1394-48-5 | [Synonyms]
Acehytisine
Kwan-fu base A
Guan-fu base A
Guan-fu base A USP/EP/BP
(2α,11α,13R)-Hetisan-2,11,13,14-tetrol 2,11-diacetate
Hetisan-2,11,13,14-tetrol,2,13-diacetate, (2a,11a,13R)-
Hetisan-2,11,13,14-tetrol, 2,13-diacetate, (2α,11α,13R)-
(2alpha,11alpha,13R)-Hetisan-2,11,13,14-tetrol 2,13-diacetate | [Molecular Formula]
C24H31NO6 | [MDL Number]
MFCD32220461 | [MOL File]
1394-48-5.mol | [Molecular Weight]
429.51 |
| Chemical Properties | Back Directory | [Boiling point ]
541.5±50.0 °C(Predicted) | [density ]
1.43±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, away from moisture and light | [form ]
Solid | [pka]
12.97±0.70(Predicted) | [color ]
White to off-white | [InChIKey]
OGNUSOJAYIHLNS-UFZRWAKRNA-N | [SMILES]
O[C@]12[C@@H]([C@]3([H])C(=C)CC41C[C@@]1([H])[C@]5([H])[C@]6(C[C@H](OC(=O)C)C[C@]5([C@]4([H])[C@@H]3O)C2N1C6)C)OC(=O)C |&1:1,2,3,10,12,14,16,22,23,25,r| |
| Hazard Information | Back Directory | [Chemical Properties]
White crystals, soluble in organic solvents such as methanol, ethanol, DMSO, etc., derived from the tuberous root of Aconitum carmichaelii (Kanbaifu), a plant of the Ranunculaceae family. | [Uses]
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]. | [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]. | [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. DOI:10.1124/dmd.114.060905
[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. DOI:10.1097/FJC.0b013e318236e380 |
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