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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Purity: ≥98%
Diflunisal (also known as MK-647; trade name Dolobid) is a novel and potent salicylate derivative with nonsteroidal anti-inflammatory and uricosuric properties, it is used alone as an analgesic and in rheumatoid arthritis patients. Diflunisal acts as a Cyclooxygenase (COX) inhibitor and was developed by Merck Sharp & Dohme in 1971 after showing promise in a research project studying more potent chemical analogs of aspirin. It is classed as a non-steroidal anti-inflammatory drug (NSAID).
| ln Vivo |
Rats given increasing dosages of diflunisal showed that the pharmacokinetics of the drug are complexly influenced by dose. Diflunisal exhibits an exponential drop in plasma concentration over time, whereas its half-life increases when the dosage is increased. When the dose was increased from 3 to 10 mg/kg, CLP dramatically dropped and subsequently stayed mostly stable throughout the 10 mg/kg to 60 mg/kg treatment range. It has been demonstrated that diflunisal binds strongly and concentration-dependently to the plasma proteins of rats. In the range of 5 to 300 μg/mL, there was an approximate 10-fold increase in the proportion of unbound diflunisal [1]. Following oral administration, diflunisal has an activity that is roughly 25 times more than aspirin, 3 times greater than glafenine, and 2 times greater than zomelar [2].
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| 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.
[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. [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 |
| Molecular Formula |
C13H8F2O3
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|---|---|
| Molecular Weight |
250.1976
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| CAS # |
22494-42-4
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| Related CAS # |
Diflunisal-d3;1286107-99-0
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| SMILES |
O=C(C1=CC(C2=CC=C(F)C=C2F)=CC=C1O)O
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| InChi Key |
HUPFGZXOMWLGNK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H8F2O3/c14-8-2-3-9(11(15)6-8)7-1-4-12(16)10(5-7)13(17)18/h1-6,16H,(H,17,18)
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| Chemical Name |
2',4'-difluoro-4-hydroxy-[1,1'-biphenyl]-3-carboxylic acid
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| Synonyms |
MK-647; MK647; MK 647; trade names: Dolobid; Dolobis; Flovacil; Fluniget; Fluodonil; Dflunisal
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~199.84 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (9.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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