Docebenone
Based on 1 Customer Validation
Docebenone (AA 861) is a potent, selective and orally active 5-LO (5-lipoxygenase) inhibitor.
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- Pureté: 99.02%
- CAS No.: 80809-81-0
- Formule: C21H26O3
- Masse moléculaire:326.43
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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5-LO |
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Cell Line
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Type | Value | Description | References |
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| HepG2 | EC50 |
28.2 μM
Compound: AA-861
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Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
7.1 μM
Compound: AA-861
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Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis
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[PMID: 20966043] |
| RBL-1 | IC50 |
2 μM
Compound: AA-861
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In vitro inhibition of RBL-1 5-lipoxygenase
In vitro inhibition of RBL-1 5-lipoxygenase
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[PMID: 3681891] |
| RBL-1 | IC50 |
9.0 x 10-8M
Compound: 1 (AA-861)
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The concentration required to reduce by 50% the amount of LTB4 formed by RBL-1 cells
The concentration required to reduce by 50% the amount of LTB4 formed by RBL-1 cells
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[PMID: 1992126] |
Treatment of trichomonads with the 5-LO inhibitor Docebenone, significantly inhibits the ability of trichomonads to secrete LTB4 compared to results for trichomonads treated with medium. Docebenone strongly abolishes the stimulatory effect of TvSP on IL-8 production[1]. Docebenone at 10-200 μM increases [Ca2+]i concentration dependently[2].
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.
Chemical Information
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CAS No. 80809-81-0
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Appearance Solid
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Masse moléculaire 326.43
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Formule C21H26O3
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Color Light yellow to yellow
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SMILES
O=C1C(CCCCC#CCCCC#CCO)=C(C)C(C(C)=C1C)=O
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Synonyms
AA 861
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvant et solubilité
DMSO : 250 mg/mL (765.86 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 6.25 mg/mL (19.15 mM); Clear solution
This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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.
Protocole
Rats[3]
Pancreatitis is induced in rats by retrograde injection of 0.4 mL/kg body wt of 6% taurocholic acid into the pancreatic duct. The animals are divided into three groups: control group; administered Docebenone in a single dose of 30 mg/kg; and administered Docebenone in a single dose of 60 mg/kg. The following parameters are examined: serum amylase, lipase, trypsin, blood sugar, and survival rate[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (270 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Nam YH, et al. Leukotriene B(4) receptors BLT1 and BLT2 are involved in interleukin-8 production in human neutrophils induced by Trichomonas vaginalis-derived secretory products. Inflamm Res. 2012 Feb;61(2):97-102. [Content Brief]
[2]. Huang JK, et al. AA-861-induced Ca(2+) mobilization in Madin Darby canine kidney cells. Toxicol Appl Pharmacol. 1999 Dec 1;161(2):202-8. [Content Brief]
[3]. Kiriyama M, et al. Protective effect of AA-861 (5-lipoxygenase inhibitor) on experimental acute necrotizing pancreatitis in rats. Int J Pancreatol. 1993 Jun;13(3):201-8. [Content Brief]
[4]. Yamamura H, et al. Effect of AA-861, a selective 5-lipoxygenase inhibitor, on models of allergy in several species. Jpn J Pharmacol. 1988 Jul;47(3):261-71. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0634 mL | 15.3172 mL | 30.6344 mL | 76.5861 mL |
| 5 mM | 0.6127 mL | 3.0634 mL | 6.1269 mL | 15.3172 mL | |
| 10 mM | 0.3063 mL | 1.5317 mL | 3.0634 mL | 7.6586 mL | |
| 15 mM | 0.2042 mL | 1.0211 mL | 2.0423 mL | 5.1057 mL | |
| 20 mM | 0.1532 mL | 0.7659 mL | 1.5317 mL | 3.8293 mL | |
| 25 mM | 0.1225 mL | 0.6127 mL | 1.2254 mL | 3.0634 mL | |
| 30 mM | 0.1021 mL | 0.5106 mL | 1.0211 mL | 2.5529 mL | |
| 40 mM | 0.0766 mL | 0.3829 mL | 0.7659 mL | 1.9147 mL | |
| 50 mM | 0.0613 mL | 0.3063 mL | 0.6127 mL | 1.5317 mL | |
| 60 mM | 0.0511 mL | 0.2553 mL | 0.5106 mL | 1.2764 mL | |
| 80 mM | 0.0383 mL | 0.1915 mL | 0.3829 mL | 0.9573 mL | |
| 100 mM | 0.0306 mL | 0.1532 mL | 0.3063 mL | 0.7659 mL |
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