bs-75591C

DATASHEET

Formulation Powder

Storage: Stable for 2 years after receipt when stored at -20°C.

Product Information:

CAS Number: 130929-57-6

Molecular formula: C14H15N3O5

Molecular weight: 305.3

Purity: >98% (HPLC)

Appearance: Yellow powder

Solubility: Soluble in DMSO (30mg/ml), dimethylformamide (30mg/ml) or ethanol (5mg/ml). Insoluble in water.

InChiKey: JRURYQJSLYLRLN-BJMVGYQFSA-N

SMILES: OC1=C(O)C([N+]([O-])=O)=CC(/C=C(C#N)/C(N(CC)CC)=O)=C1

Description:

Potent FTO (fat mass and obesity-associated gene) inhibitor for in vivo studies. FTO belongs to the Fe2+ and alpha-ketoglutarate (alpha-KG)-dependent oxygenase family. It demethylates N6-adenosine-modified (m6A) sites and N6,2'-O-dimethyladenosine-modified (m6Am) sites of mRNA. With its demethylase activity, FTO regulates the expression of some uncharacterized genes. The transcription factor FOXO1 has been shown to be a substrate of FTO. FTO demethylated m6A sites on forkhead box protein O1 (FOXO1) mRNA to up-regulate FOXO1 expression, thereby modulating gluconeogenesis and thermogenesis explaining in part the function of FTO on metabolic disorders such as obesity and diabetes. Potent selective and reversible catechol-O-methyltransferase (COMT) inhibitor, an enzyme involved in the metabolism of catecholamine neurotransmitters and related drugs. Entacapone is selective for COMT over monoamine oxidase A (MAO-A) and MAO-B and phenolsulphotransferase M (PST-M) and PST-P (IC50s = >50 µM). It is used for the treatment of Parkinson’s disease, administered concomittantly with levodopa and a decarboxylase inhibitor (e.g. carbidopa). Inhibits alpha-synuclein aggregation in an in vitro assay and blocks alpha-synuclein-induced cell death in PC-12 cells. Shown to uncouple oxidative phosphorylation and inhibit mitochondrial enzyme complexes I and IV. Antioxidant that can scavenge toxic HOCl and ONOO--species and inhibit oxidative stress-induced cell death.