| Name | Guanfu base A |
| Description | Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current. |
| In vitro | Guanfu base A does not inhibit mouse or rat CYP2Ds and shows no inhibition of human recombinant 2C8, 2C19, CYP1A2, 2A6, 3A4, or 3A5, but demonstrates slight inhibition of 2B6 and 2E1. It is a potent inhibitor of CYP2D6 with an IC50 of ~0.46 μM in HLM (Dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (Bufuralol 5 μM)[1]. Additionally, Guanfu base A inhibits HERG channel current in a concentration-, voltage-, and time-dependent manner with an IC50 of 1.64 mM, shifts the activation curve negatively, and accelerates channel inactivation without affecting the inactivation curve [2]. |
| In vivo | Beagle dogs administered Dextromethorphan (2 mg/mL) intravenously following a pretreatment with Guanfu base A injection exhibited diminished CYP2D metabolic activity. This was evidenced by the maximum concentration (Cmax) of dextrorphan being one-third compared to the saline-treated group and the area under the plasma concentration-time curve being half of that observed in the saline-treated group [1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 10 mM, Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (4.66 mM), Sonication is recommended.
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| Keywords | PotassiumChannel | Potassium Channel | KcsA | Inhibitor | inhibit | hERG | Guanfu base A | CYP2D6 |
| Inhibitors Related | Oxadiazon | Musk ketone | Naringin dihydrochalcone | Ipriflavone | Benzyl alcohol | Sudan IV | 1,8-Cineole | Tetraethylammonium bromide | Chenodeoxycholic acid | Naringin | Chlorzoxazone | Dibenzothiophene |
| Related Compound Libraries | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Traditional Chinese Medicine Monomer Library | Membrane Protein-targeted Compound Library | Selected Plant-Sourced Compound Library | Tyrosine Kinase Inhibitor Library | Natural Product Library | Anti-Inflammatory Traditional Chinese Medicine Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Ion Channel Targeted Library |
United States
