Immunology & Inflammation
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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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CCR 2 antagonist
Teijin compound 1 is a specific CCR 2 antagonist with IC50s of 24 and 180 nM in chemotaxis and binding assay, respectively.
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CCR4 antagonist
GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96????0.11.
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CCR2 antagonist
PF-4136309 is a potent, selective, and orally bioavailable CCR2 antagonist, with IC50s of 5.2 nM, 17 nM and 13 nM for human, mouse and rat CCR2.
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CCR2 antagonist
RS102895 hydrochloride is a potent CCR2 antagonist, with an IC50 of 360 nM, and shows no effect on CCR1.
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CCR9 antagonist
Vercirnon (GSK-1605786) is an orally bioavailable, selective, and potent antagonist of CCR9, with an IC50 of 10 nM, used in the research of inflammatory bowel diseases.
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non-peptide CCR1 antagonist
BX471 hydrochloride (ZK-811752 hydrochloride) is a potent, selective non-peptide CCR1 antagonist with Ki of 1 nM for human CCR1, and exhibits 250-fold selectivity for CCR1 over CCR2, CCR5 and CXCR4.
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CCR 拮抗剂
Maraviroc (UK-427857)是CCR5受体拮抗剂类别的抗逆转录病毒药物,用于治疗HIV感染。
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- Roman V Uzhachenko, .et al. Metabolic modulation by CDK4/6 inhibitor promotes chemokine-mediated recruitment of T cells into mammary tumors, Cell Rep, 2021, Apr 6;35(1):108944 PMID: 33826903
- Karampoor S, .et al. Maraviroc attenuates the pathogenesis of experimental autoimmune encephalitis, Int Immunopharmacol, 2020, Mar;80:106138 PMID: 32007705
- Taisuke Ito, .et al. CCR5 is a novel target for the treatment of experimental alopecia areata, JCIA, 2020, 22 January
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CCR5 拮抗剂
Vicriviroc Malate是CCR5拮抗剂,也是HIV-1进入靶细胞的有效抑制剂,对HIV分离株的平均IC50 = 0.46 nM,IC50 = 1?10 nM(n = 52)。
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- Tomohiro Nabekura, .et al. Effects of Antiviral Drugs on Organic Anion Transport in Human Placental BeWo Cells, Antimicrob Agents Chemother, 2015, Dec; 59(12): 7666-7670 PMID: 26416870
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CCR2 拮抗剂
INCB8761 (PF-4136309)是一种有效的,选择性的,口服可生物利用的CCR2拮抗剂。
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HCCR2 拮抗剂
INCB 3284 dimesylate是一种有效的选择性hCCR2拮抗剂,对单核细胞趋化因子分子与hCCR2的结合和趋化活性表现出强烈的拮抗作用。
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CCR2 拮抗剂
MK-0812是一种有效的选择性CCR2拮抗剂,对人单核细胞上CCR2的亲和力低,而在趋化性测定中的亲和力却低。它在临床前物种中具有良好的PK分布,并在动物模型中证明了功效。
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- Murakami K, .et al. CC chemokine ligand 2 and CXC chemokine ligand 8 as neutrophil chemoattractant factors in canine idiopathic polyarthritis, Vet Immunol Immunopathol, 2016, Dec;182:52-58 PMID: 27863550
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CCR1 拮抗剂
BX471是一种有效的选择性非肽CCR1拮抗剂(对于人CCR1,Ki = 1 nM),对CCR1的选择性是CCR2,CCR5和CXCR4的250倍。
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CCR5 拮抗剂
TAK-779是一种新颖,有效和选择性的CCR5小分子拮抗剂,在结合试验中IC50值为1.4nM。
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CCR2/CCR5 抑制剂
Cenicriviroc是用于治疗HIV感染的实验性候选药物.Cenicriviroc是CCR2和CCR5受体的抑制剂,可使其充当阻止病毒进入人体细胞的进入抑制剂。
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CCR5 entry 抑制剂
Aplaviroc是一种CCR5进入抑制剂,用于治疗HIV感染。
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CCR2 拮抗剂
RS 504393是一种选择性CCR2趋化因子受体拮抗剂(IC50值分别为98 nM和> 100 uM,分别抑制人重组CCR2b和CCR1受体)。
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CCR5 拮抗剂
Vicriviroc maleate是一种CCR5拮抗剂,在临床开发中用于治疗HIV-1的IC50为0.91 nM。
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CCR1 激动剂
NSC5844是具有C-C趋化因子受体1型(CCR1)激动特性的双喹啉化合物。
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CCR8 激动剂
ZK-756326是有效的,选择性的非肽CCR8趋化因子受体激动剂。ZK 756326抑制了CCR8配体I-309(CCL1)的结合,IC(50)值为1.8μM。
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CCR2/CCR5 拮抗剂
BMS-813160是一种有效的选择性CCR2/CCR5拮抗剂,具有潜在的免疫调节和抗肿瘤活性。
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CCR2/5 receptors 抑制剂
Cenicriviroc(TAK-652,TBR-652)是CCR2和CCR5受体的抑制剂,可使其充当防止病毒进入人细胞的进入抑制剂
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Human CCR1 拮抗剂
BI-639667 is a potent and selective antagonist of human CCR1.
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CCR2 /CCR5 dual 拮抗剂
PF-04634817 is an orally administered CCR2 and CCR5 chemokine receptor antagonist, for the treatment of diabetic nephropathies and diabetic macular oedema.
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CCR8 激动剂
LMD-009 is a selective CCR8 nonpeptide agonist. LMD-009 mediates chemotaxis, inositol phosphate accumulation, and calcium release in high potencies with EC50s from 11 to 87 nM.
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CCR2 拮抗剂
INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
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