Description
Mivotilate is a nontoxic, potent activator of the aryl hydrocarbon receptor (AhR), and acts as a hepatoprotective agent.
Product information
CAS Number: 130112-42-4
Molecular Weight: 330.45
Formula: C12H14N2O3S3
Synonym:
YH439
Chemical Name: propan-2-yl 2-(1,3-dithietan-2-ylidene)-2-[(4-methyl-1,3-thiazol-2-yl)carbamoyl]acetate
Smiles: CC1=CSC(NC(=O)C(=C2SCS2)C(=O)OC(C)C)=N1
InChiKey: WOUUWUGULFOVHG-UHFFFAOYSA-N
InChi: InChI=1S/C12H14N2O3S3/c1-6(2)17-10(16)8(11-19-5-20-11)9(15)14-12-13-7(3)4-18-12/h4,6H,5H2,1-3H3,(H,13,14,15)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
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.
References:
- 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.
- Jeong KS, et al. Transcriptional inhibition of cytochrome P4502E1 by a synthetic compound, YH439. Arch Biochem Biophys. 1996 Feb 1;326(1):137-44.
- Lee IJ, et al. Transcriptional induction of the cytochrome P4501A1 gene by a thiazolium compound, YH439. Mol Pharmacol. 1996 Jun;49(6):980-8.
Products are for research use only. Not for human use.
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