Mivotilate (YH439) (Synonyms: YH439) |
| Katalog-Nr.GC30297 |
Mivotilat (YH439) ist ein ungiftiger, starker Aktivator des Arylkohlenwasserstoffrezeptors (AhR) und wirkt als hepatoprotektives Mittel.
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Cas No.: 130112-42-4
Sample solution is provided at 25 µL, 10mM.
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Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
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[1]. Mivotilate induces cytochromes P4501A1/2 (CYP1A1/2) through the aryl hydrocarbon (Ah) receptor[3].
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[2].
[1]. Whelan F, et al. Amino acid substitutions in the aryl hydrocarbon receptor ligand binding domain reveal YH439 as an atypical AhR activator. Mol Pharmacol. 2010 Jun;77(6):1037-46. [2]. Jeong KS, et al. Transcriptional inhibition of cytochrome P4502E1 by a synthetic compound, YH439. Arch Biochem Biophys. 1996 Feb 1;326(1):137-44. [3]. Lee IJ, et al. Transcriptional induction of the cytochrome P4501A1 gene by a thiazolium compound, YH439. Mol Pharmacol. 1996 Jun;49(6):980-8.
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