Etodolac
Based on 1 Customer Validation
Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that can cross the blood-brain barrier and is a non-selective inhibitor of COX (IC50=53.5 nM)
For research use only. We do not sell to patients.
- Purity: 99.48%
- CAS No.: 41340-25-4
- Formula: C17H21NO3
- Molecular Weight:287.35
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
|
COX-2 41 nM (IC50, in CHO cells) |
COX-1 ∼50000 nM (IC50, in CHO cells) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
50 μM
Compound: Etodolac
|
TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
|
[PMID: 10991954] |
| Vero C1008 | CC50 |
569.77 μM
Compound: P2
|
Cytotoxicity in African green monkey Vero E6 cells incubated for 48 hrs by neutral red uptake assay
Cytotoxicity in African green monkey Vero E6 cells incubated for 48 hrs by neutral red uptake assay
|
[PMID: 32105468] |
| Vero C1008 | EC50 |
>100 μM
Compound: P2
|
Antiviral activity against MERS-CoV infected in African green monkey Vero E6 cells incubated for 48 hrs by neutral red uptake assay
Antiviral activity against MERS-CoV infected in African green monkey Vero E6 cells incubated for 48 hrs by neutral red uptake assay
|
[PMID: 32105468] |
Post-marketing studies demonstrated that etodolac inhibition of cyclooxygenase is somewhat COX-2 selective similar to celecoxib and other "COX-2 inhibitors." Unlike rofecoxib, both etodolac and celecoxib can fully inhibit COX-1 and are designated as having "preferential selectivity" toward COX-2. The (inactive against COX) r-enantiomer of etodolac inhibits beta-catenin levels in hepatoma cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 41340-25-4
-
Appearance Solid
-
Molecular Weight 287.35
-
Formula C17H21NO3
-
Color White to off-white
-
SMILES
O=C(O)CC(OCC1)(CC)C2=C1C3=CC=CC(CC)=C3N2
-
Synonyms
AY-24236
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : ≥ 100 mg/mL (348.01 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
* "≥" 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)
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 (8.70 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.70 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Purity & Documentation
-
Data Sheet (278 KB)
-
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
-
Handling Instructions (2659 KB)
References
[1]. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May;121(1):105-17. [Content Brief]
[2]. Ito S, Tajima K, Nogawa M et al. Etodolac, a cyclooxygenase-2 inhibitor, attenuates paclitaxel-induced peripheral neuropathy in a mouse model of mechanical allodynia. J Pharmacol Exp Ther. 2012 Jul;342(1):53-60. [Content Brief]
[3]. Yanaoka K, Oka M, Yoshimura N et al. Preventive effects of etodolac, a selective cyclooxygenase-2 inhibitor, on cancer development in extensive metaplastic gastritis, a Helicobacter pylori-negative precancerous lesion. Int J Cancer. 2010 Mar 15;126(6):1467-73. [Content Brief]
[4]. Matsuyama M, Yoshimura R, Hase T et al. Administration of the selective cyclooxygenase (COX)-2 inhibitor etodolac prolongs cardiac allograft survival in a mouse model. Mol Med Report. 2010 Sep-Oct;3(5):771-4. [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 | 3.4801 mL | 17.4004 mL | 34.8008 mL | 87.0019 mL |
| 5 mM | 0.6960 mL | 3.4801 mL | 6.9602 mL | 17.4004 mL | |
| 10 mM | 0.3480 mL | 1.7400 mL | 3.4801 mL | 8.7002 mL | |
| 15 mM | 0.2320 mL | 1.1600 mL | 2.3201 mL | 5.8001 mL | |
| 20 mM | 0.1740 mL | 0.8700 mL | 1.7400 mL | 4.3501 mL | |
| 25 mM | 0.1392 mL | 0.6960 mL | 1.3920 mL | 3.4801 mL | |
| 30 mM | 0.1160 mL | 0.5800 mL | 1.1600 mL | 2.9001 mL | |
| 40 mM | 0.0870 mL | 0.4350 mL | 0.8700 mL | 2.1750 mL | |
| 50 mM | 0.0696 mL | 0.3480 mL | 0.6960 mL | 1.7400 mL | |
| 60 mM | 0.0580 mL | 0.2900 mL | 0.5800 mL | 1.4500 mL | |
| 80 mM | 0.0435 mL | 0.2175 mL | 0.4350 mL | 1.0875 mL | |
| 100 mM | 0.0348 mL | 0.1740 mL | 0.3480 mL | 0.8700 mL |