| (S)-Flurbiprofeninhibitors of COX-1 and COX-2 |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
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| Cas No. | 51543-39-6 | SDF | Download 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 |
| Solubility | ≥10.9mg/mL in DMSO | Storage | Store at RT |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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现在有一个实验需要看一种药物与受体的结合情况，想咨询一下放射性配体受体结合实验，因为我们不具备这个实验条件，最好能外包那种
大多数药物在体内都是和特异性受体相互作用，改变细胞的生理生化功能而产生效应。目前已经确定的受体有30多种，根据受体存在的标准，受体可大致分为三类：
1．细胞膜受体：位于靶细胞膜上，如胆碱受体、肾上腺素受体、多巴胺受体、阿片受体等。
2．胞浆受体：位于靶细胞的胞浆内，如肾上腺皮质激素受体、性激素受体。
3．胞核受体：位于靶细胞的细胞核内，如甲状腺素受体。
另外也可根据受体的蛋白结构、信息转导过程、效应性质、受体位置等特点将受体分为四类：
1．含离子通道的受体（离子带受体）：如N-型乙酰胆碱受体含钠离子通道。
2．G蛋白偶联受体：M-乙酰胆碱受体、肾上腺素受体等。
3．具有酪氨酸激酶活性的受体：如胰岛素受体。
4．调节基因表达的受体（核受体）：如甾体激素受体、甲状腺激素受体等。
有些受体具有亚型，各种受体都有特定的分布部位核特定的功能，有些细胞也有多种受体。
