Nitecapone
Based on 1 Customer Validation
Nitecapone (OR-462) is an orally active and short-acting catechol-O-methyltransferase (COMT) inhibitor with gastroprotective and antioxidant properties. Nitecapone (OR-462) scavenges reactive oxygen and nitric radicals and prevents lipid peroxidation.
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- Reinheit: 98.71%
- CAS. Nr.: 116313-94-1
- Formel: C12H11NO6
- Molecular Weight:265.22
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Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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Cell Line
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Type | Value | Description | References |
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| HT-29 | EC50 |
0.82 μM
Compound: Nitecapone
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Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis
Agonist activity at GPR35 in human HT-29 cells assessed as induction of whole cell dynamic mass redistribution after 50 mins by resonant waveguide grating biosensor analysis
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10.1039/C2MD20210G |
| U2OS | EC50 |
17.1 μM
Compound: Nitecapone
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Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay
Agonist activity at GPR35 in human U2OS cells assessed as induction of beta-arrestin translocation after 5 hrs by beta-lactamase reporter gene assay
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10.1039/C2MD20210G |
Nitecapone (1-100 μM) reducesd GSH (reduced glutathione) depletion induced by ROO-by 11-38% and oxidation to oxidized glutathione (GSSG) by 32-45%[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eighty-six male Wistar rats, weighing 140-350 g[3].
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Dosage:30 mg/kg (3.3 mL/kg).
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Administration:IP, once daily for 13 days.
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Result:Selectively and specifically inhibits COMT in the peripheral tissues, and to some extent in the CNS for ca. 3 h.
Increased the thresholds for the mechanical stimuli and thus reduced mechanical allodynia.
Reduced the number of positive reactions of the ipsilateral paws when compared with the baselines in the nitecapone-pretreated rats.
Chemical Information
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CAS. Nr. 116313-94-1
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Appearance Solid
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Molecular Weight 265.22
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Formel C12H11NO6
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Color Light yellow to yellow
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SMILES
CC(/C(C(C)=O)=C/C1=CC([N+]([O-])=O)=C(O)C(O)=C1)=O
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Synonyms
OR-462
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
DMSO : 50 mg/mL (188.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (277 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Y J Suzuki, et al. Antioxidant properties of nitecapone (OR-462). Free Radic Biol Med. 1992 Nov;13(5):517-25. [Content Brief]
[3]. Oleg Kambur, et al. Nitecapone reduces development and symptoms of neuropathic pain after spinal nerve ligation in rats. Eur J Pain. 2011 Aug;15(7):732-40. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 3.7705 mL | 18.8523 mL | 37.7045 mL | 94.2614 mL |
| 5 mM | 0.7541 mL | 3.7705 mL | 7.5409 mL | 18.8523 mL | |
| 10 mM | 0.3770 mL | 1.8852 mL | 3.7705 mL | 9.4261 mL | |
| 15 mM | 0.2514 mL | 1.2568 mL | 2.5136 mL | 6.2841 mL | |
| 20 mM | 0.1885 mL | 0.9426 mL | 1.8852 mL | 4.7131 mL | |
| 25 mM | 0.1508 mL | 0.7541 mL | 1.5082 mL | 3.7705 mL | |
| 30 mM | 0.1257 mL | 0.6284 mL | 1.2568 mL | 3.1420 mL | |
| 40 mM | 0.0943 mL | 0.4713 mL | 0.9426 mL | 2.3565 mL | |
| 50 mM | 0.0754 mL | 0.3770 mL | 0.7541 mL | 1.8852 mL | |
| 60 mM | 0.0628 mL | 0.3142 mL | 0.6284 mL | 1.5710 mL | |
| 80 mM | 0.0471 mL | 0.2357 mL | 0.4713 mL | 1.1783 mL | |
| 100 mM | 0.0377 mL | 0.1885 mL | 0.3770 mL | 0.9426 mL |
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