(S)-Flurbiprofen |
カタログ番号GC18022 |
(S)-フルルビプロフェンはフルルビプロフェンの活性鏡像異性体で、COX-1 と COX-2 の IC50 値はそれぞれ 0.48 μM と 0.47 μM です 。
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Cas No.: 51543-39-6
Sample solution is provided at 25 µL, 10mM.
IC50: 0.5 μM for both COX-1 and COX-2 in guinea pig whole blood
(S)-Flurbiprofen is a dual inhibitor of COX-1 and COX-2.
Non-steroidal anti-inflammatory drugs (NSAIDs) are potent inhibitors of both COX-1 and COX-2, but are frequently supplied as racemates. In the 2-aryl propionic acid NSAID family, cyclooxygenase inhibition resides primarily in the (S)-enantiomer.
In vitro: It was found that the IC50 value of (S)-flurbiprofen was about 0.5 μM for both COX-1 and COX-2 in guinea pig whole blood [1].
In vivo: The efficacy of multiple applications of S(+)-flurbiprofen plaster (SFPP) was evaluated for the alleviation of inflammatory pain and edema in rat adjuvant-induced arthritis model. Multiple applications of SFPP could exert a significant analgesic effect from the first day of application as compared to the other NSAID drugs. In terms of paw edema, SFPP could decrease edema from the second day after application. Moreover, multiple applications of SFPP were found to be superior to those of other NSAID drugs in terms of the analgesic effect [2].
Clinical trial: Previous clinical study showed that 40 mg of S-flurbiprofen plaster showed remarkable pain relief in not only primary endpoint but also all the other endpoint with significant differences over placebo. The safety profile of S-flurbiprofen plaster 40 mg was not different from that of placebo. Thus, 40 mg was determined as the optimal tested dose [3].
References:
[1] Barnett, J. ,Chow, J.,Ives, D., et al. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system. Biochimica et Biophysica Acta 1209, 130-139 (1994).
[2] Sugimoto M et al. Topical Anti-Inflammatory and Analgesic Effects of Multiple Applications of S(+)-Flurbiprofen Plaster (SFPP) in a Rat Adjuvant-Induced Arthritis Model. Drug Dev Res. 2016 Jun;77(4):206-11.
[3] Yataba I, Otsuka N, Matsushita I, Matsumoto H, Hoshino Y. The efficacy and safety of S-flurbiprofen plaster in the treatment of knee osteoarthritis: a phase II, randomized, double-blind, placebo-controlled, dose-finding study. J Pain Res. 2017 Apr 11;10:867-880.
Cas No. | 51543-39-6 | SDF | |
Chemical Name | (S)-(+)-2-fluoro-α-methyl-4-biphenylacetic acid | ||
Canonical SMILES | FC1=CC([C@@H](C(O)=O)C)=CC=C1C2=CC=CC=C2 | ||
Formula | C15H13FO2 | M.Wt | 244.3 |
溶解度 | ≥ 10.9mg/mL in DMSO | Storage | Room temperature |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
1 mM | 4.0933 mL | 20.4666 mL | 40.9333 mL |
5 mM | 0.8187 mL | 4.0933 mL | 8.1867 mL |
10 mM | 0.4093 mL | 2.0467 mL | 4.0933 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5
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