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Mivotilate

MCE China：Mivotilate

Brand：MedChemExpress (MCE)

Cat. No.HY-100242

CAS：130112-42-4

Synonyms：YH439

Purity：99.58%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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[1]. Mivotilate induces cytochromes P4501A1/2 (CYP1A1/2) through the aryl hydrocarbon (Ah) receptor[3].

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[2].

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[2].

IC50 & Target：Aryl hydrocarbon receptor[1] 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[1]. Mivotilate induces cytochromes P4501A1/2 (CYP1A1/2) through the aryl hydrocarbon (Ah) receptor[3]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Mivotilate Related Antibodies

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References：

[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.  [Content Brief]

[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.  [Content Brief]

[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.  [Content Brief]