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Purity: ≥98%
Entacapone (OR-611) is an approved anti-PD/Parkinsons Diseasemedication acting as a specific and peripherally active catechol-O-methyltransferase (COMT) inhibitor (IC50 = 151 nM). It is used in combination with levodopa and carbidopa for treatingParkinsons disease (PD).
| ln Vitro |
Entacapone (50 μM, 48 hours) boosts the quantity of m6A on mRNA in Hep-G2 cells. It does not demonstrate any inhibitory effect on the enzymatic activity of the RNA m6A demethylase AlkB homolog 5 (ALKBH5) or the ten-eleven translocation methylcytosine dioxygenase 1 (TET1), nor does it alter the DNA methylation or histone methylation patterns in entacapone-treated Hep-G2 cells[2].
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| ln Vivo |
Entacapone produces a dose-response effect when taken orally (600 mg/kg per day for 3–9 weeks). After three weeks, the body weight of the mice was 10.1% lower than that of the controls, and their food intake was comparable.entacapone therapy resulted in a decrease in fat mass and fat mass ratio. Mice treated with entacapone also exhibit increased energy expenditure, as seen by decreases in triglycerides (10.2%), low-density lipoprotein cholesterol (31.0%), and total cholesterol (17.6%) in mice[2].
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| Animal Protocol |
Animal/Disease Models: High-fat diet-induced obese (DIO) mouse model[2]
Doses: 600 mg/kg Route of Administration: Oral administration; 600 mg/kg per day; 3-9 weeks Experimental Results: Regulated the metabolic disorders in DIO mouse. |
| References |
[1]. 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.
[2]. Shiming Peng, et al. Identification of entacapone as a chemical inhibitor of FTO mediating metabolic regulation through FOXO1. Sci Transl Med |
| Molecular Formula |
C14H15N3O5
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|---|---|
| Molecular Weight |
305.29
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| CAS # |
130929-57-6
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| Related CAS # |
Entacapone-d10;1185241-19-3;(Z)-Entacapone-d10;Entacapone sodium salt;1047659-02-8;(E)-Entacapone-d10
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| SMILES |
O=C(N(CC)CC)/C(C#N)=C/C1=CC([N+]([O-])=O)=C(O)C(O)=C1
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| InChi Key |
JRURYQJSLYLRLN-BJMVGYQFSA-N
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| InChi Code |
InChI=1S/C14H15N3O5/c1-3-16(4-2)14(20)10(8-15)5-9-6-11(17(21)22)13(19)12(18)7-9/h5-7,18-19H,3-4H2,1-2H3/b10-5+
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| Chemical Name |
(E)-2-cyano-3-(3,4-dihydroxy-5-nitrophenyl)-N,N-diethylacrylamide
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| Synonyms |
OR 611; OR611; OR-611; Comtan; Entacapone; HSDB-8251; HSDB8251; HSDB 8251;
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 61 mg/mL (199.8 mM)
Water:<1 mg/mL
Ethanol: 2 mg/mL (6.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (8.19 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.81 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 1 mg/mL (3.28 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2756 mL | 16.3779 mL | 32.7557 mL | |
| 5 mM | 0.6551 mL | 3.2756 mL | 6.5511 mL | |
| 10 mM | 0.3276 mL | 1.6378 mL | 3.2756 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06236230 | Recruiting | Drug: levodopa/carbidopa/entacapone | Parkinson Disease | Second Affiliated Hospital of Soochow University |
November 15, 2023 | Phase 4 |
| NCT04006769 | Completed | Drug: Entacapone Drug: Imatinib Mesylate |
Gastrointestinal Stromal Tumor, Malignant |
Xiangya Hospital of Central South University |
October 30, 2020 | Early Phase 1 |
| NCT00373087 | Completed | Drug: entacapone Drug: l dopa versus placebo |
Parkinson's Disease | Assistance Publique - Hôpitaux de Paris |
October 2006 | Phase 4 |
| NCT00192855 | Completed | Drug: Entacapone | Schizophrenia | Rambam Health Care Campus | June 2003 | Not Applicable |
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