Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR) , and acts as a hepatoprotective agent.
In Vitro
Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor. Mivotilate (YH439) has a novel activation mode that tolerates mutation of histidine 285 to tyrosine. Mivotilate induces cytochromes P4501A1/2 (CYP1A1/2) through the aryl hydrocarbon (Ah) receptor. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Mivotilate (YH439, 150 mg/kg, p.o.) reduces CYP2E1-mediated NDMA demethylase activity in rats, but shows no obvious effect on NADPH-dependent P450 oxidoreductase activity. Mivotilate (75-300 mg/kg) rapidly decreases immunoreactive CYP2E1 protein. Mivotilate (150 mg/kg, p.o.) inhibits the transcription of CYP2E1 in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal administration
Male outbred Sprague-Dawley rats (weighing 100-150 g) are kept on a 12-h light-dark cycle with NIH 31 autoclavable rat die and water ad libitum. After a single oral administration of Mivotilate (75, 150, and 300 mg/kg body wt, diluted in corn oil) , the animals are sacrificed at different times as indicated. Livers from control (corn oil-treated) , starved (2 days) and Mivotilate -treated animals (n = 5 per group) are immediately excised, freeze-clamped, and processed further. Another group of rats (n = 3) is treated with phenobarbital (100 mg/kg/day) by intraperitoneal injection for 2 days and sacrificed 24 h after the last dose . aladdin has not independently confirmed the accuracy of these methods. They are for reference only.
