2. Immunology/Inflammation
  3. COX
  4. Diflunisal

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.

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Diflunisal Chemical Structure

Diflunisal Chemical Structure

CAS No. : 22494-42-4

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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.

IC50 & Target[3]

COX

 

In Vivo

Administration of increasing doses of Diflunisal to rats shows that the effect of the dose on the pharmacokinetics of Diflunisal is quite complicated. The plasma concentrations of Diflunisal decline exponentially with time, albeit with a half-life that increases with increasing dose. The CLP is reduced considerably when the dose increases from 3 to 10 mg/kg and then remains relatively constant over the dose range of 10 to 60 mg/kg. Diflunisal has been shown to be highly bound to rat plasma protein and dependent on concentration. The fraction of unbound Diflunisal is increased about 10-fold over the concentration range of 5 to 300 μg/mL[1]. Diflunisal exhibits activity after oral administration with potency about 25 times greater than that of aspirin, about 3 times that of glafenine and twice that of zomepirac[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

250.20

Formula

C13H8F2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC(C2=CC=C(F)C=C2F)=CC=C1O)O
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9968 mL 19.9840 mL 39.9680 mL
5 mM 0.7994 mL 3.9968 mL 7.9936 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.

  • Molarity Calculator

  • Dilution Calculator

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 (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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Purity & Documentation

Purity: 99.91%

COA (247 KB) HNMR (119 KB) RP-HPLC (189 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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
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Diflunisal 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:

Diflunisal22494-42-4MK-647MK647MK 647COXCyclooxygenaseInhibitorinhibitorinhibit

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