2. Immunology/Inflammation Apoptosis
  3. COX Apoptosis
  4. Otenaproxesul

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.

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Otenaproxesul

Otenaproxesul Estructura química

No. CAS : 1226895-20-0

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10 mM * 1 mL in DMSO
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Other Forms of Otenaproxesul:

Otenaproxesul Related Antibodies

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Ver todos los productos específicos de isoformas COX:

Ver todas las isoformas
COX COX-1 COX-2 COX-3

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Descripciòn

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[1][4].

IC50 & Target[1]

COX-1

 

COX-2

 

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
227.6 μM
Compound: 1
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
[PMID: 28646655]
L02 IC50
3614.9 μM
Compound: 1
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
[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.

Otenaproxesul Related Antibodies

Cell Proliferation Assay[2]

Cell Line: A375 cells.
Concentration: 100 μM.
Incubation Time: 24, 48 and 72 h.
Result: Caused an inhibition of cell proliferation by 38.2%, 63.2% and 66%, respectively (P < 0.001).
In Vivo

Otenaproxesul exhibits anti-inflammatory properties similar to naproxen, but with substantially reduced gastrointestinal toxicity[1].
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.

Animal Model: Male, Wistar rats (200-225 g)[1].
Dosage: 30, 60, 120 and 2740 μmol/kg.
Administration: Orally once.
Result: Inhibited PGE2 levels.
Suppressed TXB2 synthesis.
Animal Model: Male, Wistar rats (200-225 g)[1].
Dosage: 4 μmol/kg.
Administration: Orally twice daily, on days 7 to 21.
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
Peso molecular

365.45

Fòrmula

C21H19NO3S
No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

COC1=CC=C(C=C(C(C)C(OC2=CC=C(C(N)=S)C=C2)=O)C=C3)C3=C1
Envío

Room temperature in continental US; may vary elsewhere.
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7364 mL 13.6818 mL 27.3635 mL
5 mM 0.5473 mL 2.7364 mL 5.4727 mL
View the 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.

  • Calculadora de molaridad

  • Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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Referencias

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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Otenaproxesul Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Otenaproxesul1226895-20-0ATB-346ATB346ATB 346COXApoptosisCyclooxygenaseColorectalcancerPGE2TXB2melanomaperiodontitisbonelossInhibitorinhibitorinhibit

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Nombre del producto:
Otenaproxesul
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HY-15028
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