Immunology & Inflammation
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COX/LOX 抑制剂
Licofelone是一种COX/LOX双重抑制剂,被认为是治疗骨关节炎的药物。它可能会降低与其他仅抑制COX(环氧合酶)的非甾体类抗炎药有关的胃肠道毒性。利福非酮是第一种同时抑制两者的药物。
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- Silke Neumann, .et al. Improved Antitumor Activity of a Therapeutic Melanoma Vaccine through the Use of the Dual COX-2/5-LO Inhibitor Licofelone, Front Immunol, 2016, 7: 537 PMID: 27994586
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COX 抑制剂
Diclofenac Sodium是一种非选择性的COX抑制剂,完整细胞中的COX-1和-2的IC50分别为0.5μg/ml和0.5μg/ml,作用于绵羊COX-1和COX-2, IC50分别为60和220 nM,用作非甾体类抗炎药(NSAID)来减轻疼痛和减轻疼痛 肿胀发炎。
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ATB-337是H2S供体和NSAID双氯芬酸的杂合分子。
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COX-2 抑制剂
Rofecoxib (Vioxx)是一种COX-2抑制剂,IC50值为18 nM。
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Phenacetin是一种非阿片类镇痛药,无抗炎特性。
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COX 抑制剂
Indomethacin (Indocid, Indocin)是一种非选择性COX1和COX2抑制剂,IC50分别为0.1 μg/mL和5 μg/mL。吲哚美辛(吲哚满,吲哚满)是一种非甾体抗炎药,通常用于减轻发热、疼痛、僵硬和肿胀。
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- Reiko Watanabe, .et al. Development of an In Silico Prediction Model for P-glycoprotein Efflux Potential in Brain Capillary Endothelial Cells toward the Prediction of Brain Penetration, J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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COX 抑制剂
Phenylbutazone (Butazolidin,Butatron)是一种具有研究意义的化合物,它是一种抗炎和抗增殖剂。
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COX 抑制剂
Piroxicam (Feldene)是前列腺素合成的有效抑制剂,并且是Cox-1和Cox-2抑制剂。
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COX-2 抑制剂
Iguratimod (T 614)是一种抗风湿剂,能够有效地抑制COX-2的活性,IC50值为20 μM (7.7 μg/mL),而对 COX-1 无作用;Iguratimod同时为巨噬细胞移动抑制因子 (MIF) 抑制剂,IC50值为6.81 μM。
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Jaceosidin是一种来源于艾蒿的药理活性黄酮,通过阻断培养的人乳腺上皮细胞中erk-1和-2的磷酸化来抑制佛波酯诱导的cox-2和MMP-9的上调。
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COX 抑制剂
(S)-(+)-Flurbiprofen是一种非选择性的Cox-1和Cox-2抑制剂。
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- Xing Jin, .et al. Enantioselective analysis of ketoprofen in human saliva by liquid chromatography/tandem mass spectrometry with chiral derivatization, Microchemical Journal, 2018, 143: 280-285
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COX-2 抑制剂?
NS-398是具有镇痛和解热作用的非甾体类抗炎药,可选择性抑制前列腺素G / H合酶2 /环氧合酶2(COX-2)活性,IC50为3.8μM,对COX无影响
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COX-2 抑制剂
Bromfenac sodium是一种局部选择性环氧合酶(COX)-2抑制剂
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COX 抑制剂
Acetaminophen (paracetamol) 是选择性环氧合酶-2 (COX-2) 的抑制剂,IC50 值为 25.8 μM。Acetaminophen 是一种有效的肝 N-乙酰转移酶 2 (NAT2) 抑制剂。它是广泛使用的解热和止痛药。
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- Takashi Azuma, .et al. Removal of pharmaceuticals in water by introduction of ozonated microbubbles, SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. Distribution of six anticancer drugs and a variety of other pharmaceuticals, and their sorption onto sediments, in an urban Japanese river, Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. Detection of pharmaceuticals and phytochemicals together with their metabolites in hospital effluents in Japan, and their contribution to sewage treatment plant influents, Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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COX 抑制剂
Naproxen sodium是一种非选择性的环氧合酶(COX)抑制剂,具有抗炎,解热和镇痛作用。对秋水仙碱引起的认知障碍和氧化应激具有神经保护作用。
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COX-2 抑制剂
FK3311是一种可渗透细胞且可口服的磺酰苯胺,可作为选择性COX-2抑制剂和NSAID。
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COX-2 抑制剂
伐地考昔(Valdecoxib),也称为SC-65872,是一种非甾体类抗炎药(NSAID),用于治疗骨关节炎,类风湿性关节炎以及痛经和月经症状。 它是一种选择性的环氧合酶2(COX-2)抑制剂,IC50为5nM。
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COX-2 抑制剂
Parecoxib是一种有效的选择性COX-2抑制剂。
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Fenbufen是一种具有消炎,镇痛和解热活性的口服活性苯基链烷酸衍生物。
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COX 抑制剂
Diflunisal是具有止痛和抗炎活性的水杨酸衍生物。
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COX 抑制剂
Amfenac Sodium Monohydrate是一种非甾体止痛消炎药,带有乙酸部分。COX1和COX2的IC50值分别为250 nM和150 nM。
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COX 抑制剂
Ampiroxicam是一种非选择性的环氧合酶抑制剂,被用作抗炎药。
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COX-2 抑制剂
Carprofen通过抑制COX-2和其他炎症性前列腺素来减轻炎症,不干扰COX-1活性。
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COX and lipo-oxygenase 抑制剂
Timegadine被发现是一种有效的竞争性环加氧酶(COX)和脂加氧酶抑制剂,IC50的范围从5 nM(洗兔血小板)到20μM(大鼠脑)。在马血小板匀浆的细胞溶质级分和洗涤过的兔血小板中,脂氧化酶的浓度为100μM和100μM。
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COX 抑制剂
Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
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COX-2 抑制剂
Firocoxib is a non-steroidal anti-inflammatory drug of the COX-2 inhibitor class, currently approved for use in dogs and horses.
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COX-2 抑制剂
Aceclofenac is a cyclooxygenase-2 inhibitor used to treat osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
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COX 抑制剂
Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
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COX-2 抑制剂
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect.
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NSAID and COX-2 抑制剂
Deracoxib is an NSAID and COX-2 inhibitor used to treat osteoarthritis. It induces cell cycle arrest and apoptosis in mammary tumor cells, decreases platelet aggregation, and lowers inflammatory responses.
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COX-2 抑制剂
Bromfenac Sodium Sesquihydrate is a nonsteroidal anti-inflammatory drug (NSAID), which inhibits cyclooxygenase II (COX-2).
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COX 抑制剂
Dipyrone, also known as Anador and NSC-73205, is a nonsteroidal anti-inflammatory drug used to treat pain (postoperative, colic, cancer, and migraine).
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Hsp90/SRC/COX-2 抑制剂
Radicicol是Hsp90,SRC和Cox-2的有效抑制剂。
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COX 抑制剂/histamine H1 receptor 激动剂
Fexofenadine Hydrochloride是一种抗组胺药,可抑制Cox-1,Cox-2,并且是组胺H1受体激动剂,IC50为246 nM。
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COX/5-LOX 抑制剂
Tepoxalin是花生四烯酸代谢的双重环氧合酶/5-脂氧合酶抑制剂,具有有效的抗炎活性和良好的胃肠道功能。
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COX 抑制剂
Flufenamic acid是一种非甾体类抗炎药(NSAID)。抑制钙激活的氯离子通道(CaCC)。也增加通过TRPC6通道的电流,并抑制通过TRPC3和TRPC7通道的电流。
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COX 抑制剂
Pranoprofen是一种用于眼科的非甾体类抗炎药。
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COX-1 抑制剂
(-)-Epicatechin是绿茶的天然产物。(-)表儿茶素是cox-1的抑制剂。
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- A S D'Costa, .et al. Inhibition of starch digestion by flavonoids: Role of flavonoid-amylase binding kinetics, Food Chem, 2020, Oct 1;341(Pt 2):128256 PMID: 33035827
- Mihaela Tudorache, .et al. Phenolic compounds mediate aggregation of water-soluble polysaccharides and change their rheological properties: Effect of different phenolic compounds, Food Hydrocoll, 2019, 97, Dec, 105193
- Md Shajedul Islam, .et al. UV-C irradiation as an alternative disinfection technique: Study of its effect on polyphenols and antioxidant activity of apple juice, Innovative food science & emerging technologies, 2016, v.34 pp. 344-351
- Islam MS, .et al. Effect of UV Irradiation on the Nutritional Quality and Cytotoxicity of Apple Juice, J Agric Food Chem, 2016, Oct 10 PMID: 27632812
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COX-2 抑制剂
ATB-346具有类似于萘普生的抗炎特性,但其胃肠道毒性显着降低。
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COX 抑制剂
Meclofenamate Sodium是一种双重COX-1/COX-2抑制剂,IC50为40 nM和50 nM。
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COX-1 抑制剂
Paradol是几内亚胡椒(Aframomum melegueta)种子的活性风味成分。已发现Paradol具有抗氧化和抗肿瘤的促进作用。
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- Taurin Hughes, .et al. Inhibition of Escherichia coli ATP synthase by dietary ginger phenolics, Int J Biol Macromol, 2021, Jul 1;182:2130-2143 PMID: 34087308
- Lihan Zhao, .et al. Efficacy based ginger fingerprinting reveals potential antiproliferative analytes for triple negative breast cancer, Sci Rep, 2020, Nov 5;10(1):19182 PMID: 33154433
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COX-2 抑制剂
Etoricoxib特异性结合并抑制环氧合酶2(COX-2),从而抑制花生四烯酸向前列腺素的转化。抑制COX-2可以诱导细胞凋亡并抑制肿瘤细胞的增殖和血管生成。
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COX 抑制剂
Xanthohumol是一种来自啤酒花的烯丙基查尔酮,可抑制COX-1和COX-2活性并显示化学预防作用。
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COX-1 抑制剂
SC 560是一种COX-1选择性抑制剂,IC50 值为9 nM。可以用作研究COX-1衍生的PG在炎症和疼痛中的作用的药理学工具。
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COX inhibitor
Etodolac (AY-24236) is a non-steroidal anti-inflammatory compound that is a non-selective inhibitor of COX (IC50=53.5 nM).
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- Paul Mark Medina, .et al. Revealing the anticancer potential of candidate drugs in vivo using Caenorhabditis elegans mutant strains, Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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COX-1 inhibitor
Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 ?M and 1.2 ?M for COX-1 and COX-2, respectively.
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COX-2 inhibitor
GW406381, a highly selective cyclooxygenase-2 (COX-2) inhibitor, attenuates spontaneous ectopic discharge in sural nerves of rats following chronic constriction injury.
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COX/LOX inhibitor
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 ?M??
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COX-1/COX-2 inhibitor
Aspirin is a non-selective and irreversible inhibitor of COX-1 and COX-2 with IC50s of 5 and 210 μg/mL.
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COX-1 and COX-2 inhibitor
Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
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