1. Immunology/Inflammation
  2. COX

Diflunisal (Synonyms: MK-647)

Cat. No.: HY-18342 Purity: 99.37%
Handling Instructions

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.

Diflunisal Chemical Structure

Diflunisal Chemical Structure

CAS No. : 22494-42-4

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
100 mg USD 70 In-stock
Estimated Time of Arrival: December 31
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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

Target: Cyclooxygenase

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].

Clinical Trial
Solvent & Solubility
In Vitro: 

10 mM in 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
10 mM 0.3997 mL 1.9984 mL 3.9968 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

250.20

Formula

C₁₃H₈F₂O₃

CAS No.

22494-42-4

SMILES

O=C(C1=CC(C2=CC=C(F)C=C2F)=CC=C1O)O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Purity: 99.37%

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Product Name:
Diflunisal
Cat. No.:
HY-18342
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Diflunisal

Cat. No.: HY-18342