Guanfu base A is a potent noncompetitive inhibitor of CYP2D6, with a Ki value of 1.20 μM in human liver microsomes and 0.37 μM for the recombinant form. This antiarrhythmic alkaloid, derived from Aconitum coreanum, also exhibits competitive inhibition of CYP2D in monkey and dog microsomes, with Ki values of 0.38 μM and 2.4 μM, respectively. In addition to its CYP2D6 inhibitory activity, Guanfu base A demonstrates the ability to inhibit HERG channel current, making it relevant for studies in drug metabolism and cardiac electrophysiology.
Guanfu base A is a potent noncompetitive inhibitor of CYP2D6, with a Ki value of 1.20 μM in human liver microsomes and 0.37 μM for the recombinant form. This antiarrhythmic alkaloid, derived from Aconitum coreanum, also exhibits competitive inhibition of CYP2D in monkey and dog microsomes, with Ki values of 0.38 μM and 2.4 μM, respectively. In addition to its CYP2D6 inhibitory activity, Guanfu base A demonstrates the ability to inhibit HERG channel current, making it relevant for studies in drug metabolism and cardiac electrophysiology.
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