Guan-fu base A, Inhibitor

Guan-fu base A

Cat. Num. AAA5759003

• Purity: 99.71%
• Synonyms: Guan-fu base A; Guanfu base A; inhibitor

• Purity/Purification: 99.71%
• Form/Format: Solid. Powder

• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• Formula: C24H31NO6
• SMILES: CC(=O)O[C@H]1C[C@@]2(CN3[C@@H]4[C@H]2[C@]5(C1)[C@H]3[C@]6(C([C@H]7[C@H]([C@@H]5[C@]6(C4)CC7=C)O)OC(=O)C)O)C
• CAS Number: 1394-48-5
• Target & IC50: CYP2D6: ic50 0.37uM (Ki, cell free); HERG channel
• In Vitro: Beagle dogs treated intravenously with Dextromethorphan (2mg/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].
• Preparation and Storage: Store at -20 degree C for 3 years powder; -80 degree C for 2 years in solvent

Structure

Related Product Information for Guan-fu base A, inhibitor

Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20uM in HLMs; Ki: 0.37 uM for rCYP2D6). It also inhibits HERG channel current.

Product Categories/Family for Guan-fu base A, inhibitor

Metabolism; P450; Membrane Transporter/Ion Channel

References

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.
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.
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.
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.