| Description | (-)-Cephaeline (dihydrochloride) is an enantiomer of Cephaeline. Cephaeline is a selective CYP2D6 inhibitor (IC50: 121 μM). |
| In vitro | IC50 of Cephaeline against CYP2C9, CYP2D6, and CYP3A4 is over 1000, 121 and 1000 μM, respectively. Further experiments are performed to determine inhibition constants (Ki) for Cephaeline on the CYP2D6 and CYP3A4 activities Graphic analysis of Dixon plots at various Cephaeline concentrations for each of the two CYP enzyme assays yield Kis of 54 and 355 μM for CYP2D6 and CYP3A4, respectively. |
| Target activity | CYP2D6:121 μM |
| Synonyms | (-)-Cephaeline dihydrochloride, 盐酸吐根酚碱, NSC 32944 |
| molecular weight | 539.54 |
| Molecular formula | C28H40Cl2N2O4 |
| CAS | 5853-29-2 |
| Storage | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 80mg/ml H2O: 60mg/ml |
| References | 1. Asano T, et al. Metabolism of ipecac alkaloids Cephaeline and Emetine by human hepatic microsomal cytochrome P450s, and their inhibitory effects on P450 enzyme activities. Biol Pharm Bull. 2001 Jun;24(6):678-82. |