Otenaproxesul
Based on 1 Customer Validation
Otenaproxesul (ATB-346), an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2). Otenaproxesul possesses antiinflammatory and antinociceptive activities.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 98.69%
- No. CAS: 1226895-20-0
- Fòrmula: C21H19NO3S
- Peso molecular:365.45
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
COX-1 |
COX-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | IC50 |
227.6 μM
Compound: 1
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Cytotoxicity against human HepG2 cells assessed as reduction in cell survival after 24 hrs by MTT assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell survival after 24 hrs by MTT assay
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[PMID: 28646655] |
| L02 | IC50 |
3614.9 μM
Compound: 1
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Cytotoxicity against human LO2 cells assessed as reduction in cell survival after 24 hrs by MTT assay
Cytotoxicity against human LO2 cells assessed as reduction in cell survival after 24 hrs by MTT assay
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[PMID: 28646655] |
In Vitro
Otenaproxesul (100 μM) inhibits human melanoma cell proliferation by inhibiting pro-survival pathways associated with NF-B and Akt activation[2].
Otenaproxesul (100 μM) induces apoptosis of human melanoma cells[2].
Otenaproxesul (100 M) causes inhibition of IkB degradation and of NF-kB nuclear translocation as demonstrated by a reduction in band intensity of the p65 subunit in A375 cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375 cells.
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Concentration:100 μM.
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Incubation Time:24, 48 and 72 h.
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Result:Caused an inhibition of cell proliferation by 38.2%, 63.2% and 66%, respectively (P < 0.001).
In Vivo
Otenaproxesul (orally, 43 μmol/kg) inhibits growth of melanoma tumors in vivo and reduce plasma levels of melanoma-associated chemokines[2].
Otenaproxesul (orally, 16 mg/kg) results in significant inhibition of bone defect and other histological characteristics (such as flatness of the gingival epithelium, chronic inflammatory cell infiltration and loss of connective tissue in the gingival papillae). Otenaproxesul inhibits the increase of gingival IL-1β and IL-6 secondary to periodontitis, but IL-10 is unaffected[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male, Wistar rats (200-225 g)[1].
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Dosage:30, 60, 120 and 2740 μmol/kg.
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Administration:Orally once.
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Result:Inhibited PGE2 levels.
Suppressed TXB2 synthesis.
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Animal Model:Male, Wistar rats (200-225 g)[1].
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Dosage:4 μmol/kg.
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Administration:Orally twice daily, on days 7 to 21.
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Result:Significantly reduced paw oedema at days 14 and 21 (*P < 0.05 vs. the vehicle-treated group).
Caused markedly less gastric damage at all doses tested than naproxen.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1226895-20-0
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Appearance Solid
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Peso molecular 365.45
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Fòrmula C21H19NO3S
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Color Light yellow to yellow
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SMILES
COC1=CC=C(C=C(C(C)C(OC2=CC=C(C(N)=S)C=C2)=O)C=C3)C3=C1
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Synonyms
ATB-346
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvente y solubilidad
In Vitro:
DMSO : ≥ 51.6 mg/mL (141.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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)
In Vivo:
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: ≥ 2.5 mg/mL (6.84 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
In Vivo Dissolution Calculator
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.
Pureza y Documentación
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Ficha de datos (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. John L Wallace, et al. Markedly reduced toxicity of a hydrogen sulphide-releasing derivative of naproxen (ATB-346). Br J Pharmacol. 2010 Mar;159(6):1236-46. [Content Brief]
[2]. Paola De Cicco, et al. ATB-346, a novel hydrogen sulfide-releasing anti-inflammatory drug, induces apoptosis of human melanoma cells and inhibits melanoma development in vivo. Pharmacol Res. 2016 Dec;114:67-73. [Content Brief]
[3]. Bruno Schneider Herrera, et al. The H2S-releasing naproxen derivative, ATB-346, inhibits alveolar bone loss and inflammation in rats with ligature-induced periodontitis. Med Gas Res. 2015 Feb 27;5:4. [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 | 2.7364 mL | 13.6818 mL | 27.3635 mL | 68.4088 mL |
| 5 mM | 0.5473 mL | 2.7364 mL | 5.4727 mL | 13.6818 mL | |
| 10 mM | 0.2736 mL | 1.3682 mL | 2.7364 mL | 6.8409 mL | |
| 15 mM | 0.1824 mL | 0.9121 mL | 1.8242 mL | 4.5606 mL | |
| 20 mM | 0.1368 mL | 0.6841 mL | 1.3682 mL | 3.4204 mL | |
| 25 mM | 0.1095 mL | 0.5473 mL | 1.0945 mL | 2.7364 mL | |
| 30 mM | 0.0912 mL | 0.4561 mL | 0.9121 mL | 2.2803 mL | |
| 40 mM | 0.0684 mL | 0.3420 mL | 0.6841 mL | 1.7102 mL | |
| 50 mM | 0.0547 mL | 0.2736 mL | 0.5473 mL | 1.3682 mL | |
| 60 mM | 0.0456 mL | 0.2280 mL | 0.4561 mL | 1.1401 mL | |
| 80 mM | 0.0342 mL | 0.1710 mL | 0.3420 mL | 0.8551 mL | |
| 100 mM | 0.0274 mL | 0.1368 mL | 0.2736 mL | 0.6841 mL |
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