Product Name
Cephaeline dihydrochloride
Synonyms
(-)-Cephaeline dihydrochloride; NSC 32944
Description
Cephaeline dihydrochloride is a selective CYP2D6 inhibtor with an IC50 of 121 μM.
Structural Formula
Cephaeline dihydrochloride
Solubility
DMSO : 250 mg/mL(463.37 mM;Need ultrasonic) H2O : 125 mg/mL(231.68 mM;Need ultrasonic)
Source
Plants >other families
Storage
4℃, sealed storage, away from moisture and light
Shipping
Room temperature in continental US; may vary elsewhere.
SMILES
Cl[H].CC[C@@H](CN1CC2)[C@H](C[C@@]1([H])C3=C2C=C(OC)C(OC)=C3)C[C@]4([H])C5=CC(OC)=C(O)C=C5CCN4.Cl[H]
In Vitro
CYP2D6 reveals the highest metabolic activity for the generation of 9-O-demethylEmetine, whereas this enzyme also shows a significant metabolic activity for the generation of Cephaeline. The IC50s 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.
Datasheet 
