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Entacapone-d10

CAT: 0804-HY-14280S-01Size: 500 µgDry Ice: NoHazardous: No
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CAT#:0804-HY-14280S-01Size:500 µg
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Description
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM) . Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].
CAS Number
1185241-19-3
UNSPSC
12352005
Target
COMT
Type
Isotope-Labeled Compounds
Related Pathways
Metabolic Enzyme/Protease; Neuronal Signaling
Field of Research
Neurological Disease
Purity
98.0
Solubility
10 mM in DMSO|DMSO : 33.33mg/mL (ultrasonic) |H2O : 2mg/mL (ultrasonic; adjust pH to 10 with NaOH)
Smiles
OC1=C([N+]([O-])=O)C=C(/C=C(C#N)/C(N(C([2H])([2H])C([2H])([2H])[2H])C([2H])([2H])C([2H])([2H])[2H])=O)C=C1O
Molecular Formula
C14H5D10N3O5
Molecular Weight
315.35
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]E Nissinen, et al. Biochemical and pharmacological properties of a peripherally acting catechol-O-methyltransferase inhibitor entacapone. Naunyn Schmiedebergs Arch Pharmacol. 1992 Sep;346 (3) :262-6.|[3]Shiming Peng, et al. Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. Sci Transl Med
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, sealed storage, away from moisture)
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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