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(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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(S)-Flurbiprofen 化学構造

Cas No.: 51543-39-6

サイズ 価格 在庫数 個数
100mg
$68.00
在庫あり
10mM (in 1mL DMSO)
$75.00
在庫あり
250mg
$140.00
在庫あり
500mg
$243.00
在庫あり

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Sample solution is provided at 25 µL, 10mM.

Description of (S)-Flurbiprofen

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.

Chemical Properties of (S)-Flurbiprofen

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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of (S)-Flurbiprofen

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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
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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.

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Average Rating: 5 ★★★★★ (Based on Reviews and 40 reference(s) in Google Scholar.)

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