Diflunisal
Based on 1 publication(s) in Google Scholar
Diflunisal (MK-647) is a salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, which is used alone as an analgesic and in rheumatoid arthritis patients. The mechanism of action of diflunisal is as a Cyclooxygenase (COX) Inhibitor.
For research use only. We do not sell to patients.
- Purity: 99.82%
- CAS No.: 22494-42-4
- Formula: C13H8F2O3
- Molecular Weight:250.20
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Diflunisal
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Biological Activity
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COX |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.85 μM
Compound: Diflunisal
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TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells
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[PMID: 10991954] |
| Macrophage cell line | IC50 |
53 μM
Compound: 1
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Cytotoxicity against human PBMC-differentiated macrophages treated for 24 hrs followed by compound washout and measured after 48 hrs by MTT assay
Cytotoxicity against human PBMC-differentiated macrophages treated for 24 hrs followed by compound washout and measured after 48 hrs by MTT assay
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[PMID: 30108991] |
| Mahlavu | IC50 |
51.7 μM
Compound: Diflunisal
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Cytotoxicity against human Mahlavu cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
Cytotoxicity against human Mahlavu cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay
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[PMID: 26695731] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 22494-42-4
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Appearance Solid
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Molecular Weight 250.20
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Formula C13H8F2O3
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Color White to off-white
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SMILES
O=C(C1=CC(C2=CC=C(F)C=C2F)=CC=C1O)O
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Synonyms
MK-647
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Ther
RAC1 directly phosphorylates both PKM2 and FBP1 to promote radioresistance in hepatocellular carcinoma. [Abstract]2025 Nov 7:S1525-0016(25)00870-6. PMID: 41204670
Solvent & Solubility
DMSO : 50 mg/mL (199.84 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: ≥ 2.5 mg/mL (9.99 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.
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.
Protocol
Rats[1]
For the study of dose dependency, Diflunisal is administered by i.a. injection in doses of 3, 10, 30 and 60 mg/kg (1.5, 5, 15 and 30 mg/mL dosing solution in 0.1 M NaHCO3). The infusion studies consist of a bolus injection of Diflunisal followed immediately by a 7-hr infusion at a constant rate. Seven groups of rats are included in the infusion studies. The loading doses used are 2, 3, 5, 10, 25, 50 and 80 mg/kg and their corresponding infusion rates are 3, 4.5, 9, 18, 36, 72 and 144 μg/min (0.576 mL/hr of seven different dosing solutions: 0.31, 0.47, 0.94, 1.88, 3.75, 7.5 and 15 mg/mL in 0.1 M NaHCO3). Blood samples are collected serially at appropriate times for the dose-dependency studies, but collected hourly for the infusion studies. Plasma is obtained immediately by centrifugation of blood samples and extracted with acetonitrile and then frozen (-20°C) until assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (557 KB)
- English - EN (557 KB)
- Français - FR (557 KB)
- Deutsch - DE (557 KB)
- Norwegian - NO (557 KB)
- Español - ES (557 KB)
- Swedish - SV (557 KB)
- Italian - IT (557 KB)
- Korean - KR (557 KB)
- Portuguese - PT (557 KB)
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Handling Instructions (2659 KB)
References
[1]. Lin JH, et al. Dose-dependent pharmacokinetics of diflunisal in rats: dual effects of protein binding and metabolism. J Pharmacol Exp Ther. 1985 Nov;235(2):402-6. [Content Brief]
[2]. Winter CA, et al. Analgesic activity of diflunisal [MK-647; 5-(2,4-difluorophenyl)salicylic acid] in rats with hyperalgesia induced by Freund's adjuvant. J Pharmacol Exp Ther. 1979 Dec;211(3):678-85. [Content Brief]
[3]. Cappon GD, et al. Relationship between cyclooxygenase 1 and 2 selective inhibitors and fetal development when administered to rats and rabbits during the sensitive periods for heart development and midline closure. Birth Defects Res B Dev Reprod Toxicol. 2003 Feb;68(1):47-56. [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 | 3.9968 mL | 19.9840 mL | 39.9680 mL | 99.9201 mL |
| 5 mM | 0.7994 mL | 3.9968 mL | 7.9936 mL | 19.9840 mL | |
| 10 mM | 0.3997 mL | 1.9984 mL | 3.9968 mL | 9.9920 mL | |
| 15 mM | 0.2665 mL | 1.3323 mL | 2.6645 mL | 6.6613 mL | |
| 20 mM | 0.1998 mL | 0.9992 mL | 1.9984 mL | 4.9960 mL | |
| 25 mM | 0.1599 mL | 0.7994 mL | 1.5987 mL | 3.9968 mL | |
| 30 mM | 0.1332 mL | 0.6661 mL | 1.3323 mL | 3.3307 mL | |
| 40 mM | 0.0999 mL | 0.4996 mL | 0.9992 mL | 2.4980 mL | |
| 50 mM | 0.0799 mL | 0.3997 mL | 0.7994 mL | 1.9984 mL | |
| 60 mM | 0.0666 mL | 0.3331 mL | 0.6661 mL | 1.6653 mL | |
| 80 mM | 0.0500 mL | 0.2498 mL | 0.4996 mL | 1.2490 mL | |
| 100 mM | 0.0400 mL | 0.1998 mL | 0.3997 mL | 0.9992 mL |
Diflunisal Related Classifications
HY-18342 Related Classifications
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