C5264-500mg | (S)-Flurbiprofen [51543-39-6] Clinisciences

Background

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

Storage	Store at RT
M.Wt	244.3
Cas No.	51543-39-6
Formula	C₁₅H₁₃FO₂
Solubility	insoluble in H2O; ≥10.9 mg/mL in DMSO; ≥69.1 mg/mL in EtOH
Chemical Name	(S)-(+)-2-fluoro-α-methyl-4-biphenylacetic acid
SDF	Download SDF
Canonical SMILES	FC1=CC([C@@H](C(O)=O)C)=CC=C1C2=CC=CC=C2
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Purity = 98.00%

COA (Certificate Of Analysis)
MSDS (Material Safety Data Sheet)

Chemical structure

(S)-Flurbiprofen [51543-39-6]

Referentie C5264-500mg

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Background

Chemical Properties

Quality Control

Chemical structure