Biochem/physiol Actions

Primary TargetCytochrome P450 (CYP)-inducing agents

Cell permeable: no

Reversible: no

Product does not compete with ATP.

General description

A highly potent inducer of phenobarbital-like class of cytochrome P450 (CYP) enzymes. A tumor promoter that induces hepatocyte proliferation, independent of the presence of cytokines or transcription factors. Activates orphan nuclear receptors mCAR (mouse constitutive androstane receptor) and hPXR (human pregane X receptor), but has little or no effect on hCAR and mPXR. Also suppresses the expression of multi-drug resistance genes mdr2 and mdr3 in mouse liver.

The most potent known member of the phenobarbital-like class of cytochrome P450 (CYP)-inducing agents. Acts as a tumor promoter of murine hepatocarcinogenesis; activates orphan nuclear receptors mCAR (mouse Constitutive Androstane Receptor) and hPXR (human Pregnane X Receptor), but has little or no activity on hCAR and mPXR. Also suppresses the multidrug resistance gene expression in the mouse liver.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Ledda-Columbano, G.M., et al. 2000. Am. J. Pathol.156, 91.Moore, L.B., et al. 2000. J. Biol. Chem.275, 15122.Tzameli, I., et al. 2000. Mol. Cell. Biol.20, 2951.Forman, B.M., et al. 1998. Nature395, 612.Honkakoski, P., et al. 1998. Mol. Pharmacol.53, 597.Russell, A.L., et al. 1994. Int. J. Cancer58, 550.Smith, G., et al. 1993. Biochem. J.289, 807.Dargani, T.A., et al. 1990. Carcinogenesis11, 1153.Poland, A., et al. 1980. Mol. Pharmacol.18, 571.

Packaging

Packaged under inert gas

25 mg in Plastic ampoule

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Warning

Toxicity: Carcinogenic / Teratogenic (D)