product name Entacapone
Description: Entacapone inhibits catechol-O-methyltransferase(COMT) with IC50 of 151 nM. Entacapone has been used as an adjunct to standard levodopa-dopa decarboxylase inhibitor therapy in patients with Parkinson’s disease (PD), for its abilities to increase the bioavailability of levodopa by inhibiting the generation of 3-O-methyldopa and to prolong the duration and clinical benefit of levodopa.
References: Eur J Clin Pharmacol. 1998 May;54(3):215-9; J Biol Chem. 2010 May 14;285(20):14941-54.
305.29
Formula
C14H15N3O5
CAS No.
130929-57-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 61 mg/mL (199.8 mM)
Water: <1 mg/mL
Ethanol: 2 mg/mL (6.5 mM)
Solubility (In vivo)
Synonyms
OR-611
other peoduct :
| In Vitro |
In vitro activity: Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but entacapone is more active than tolcapone in those tissues. Entacapone (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells. Kinase Assay: Entacapone is a second-generation catechol-O-methyltransferase (COMT) inhibitor that potently inhibits rat liver total COMT with the half maximal inhibition concentration IC50 and inhibition constant Ki values of 20.1 nM and 10.7 nM respectively. The IC50 values of entacapone against rate liver soluble COMT (S-COMT) and rat liver membrane-bound COMT (MB-COMT) are 14.3 nM and 73.3 nM respectively Cell Assay: Entacapone inhibits catechol-O-methyltransferase(COMT) with similar IC50 in different tissues including live, duodenum, kidney and lung, but entacapone is more active than tolcapone in those tissues. Entacapone (< 100 μM) is a potent inhibitor of α-syn and β-amyloid (Aβ) oligomerization and fibrillogenesis, and also protects against extracellular toxicity induced by the aggregation of both proteins in PC12 cells. |
|---|---|
| In Vivo | Levodopa/carbidopa/entacapone has been shown to improve the pharmacokinetic profile of levodopa and provide superior symptomatic control compared with conventional levodopa/dopa decarboxylase inhibitor therapy. We report four case histories describing clinical experience of using levodopa/carbidopa/entacapone 200/50/200 mg, one of the latest doses of this formulation, in a range of patients with Parkinsons disease. These cases illustrate that levodopa/carbidopa/entacapone 200/50/200 mg provides improvements in symptomatic control. |
| Animal model | |
| Formulation & Dosage | |
| References | Eur J Clin Pharmacol. 1998 May;54(3):215-9; J Biol Chem. 2010 May 14;285(20):14941-54. |
