Immunology & Inflammation
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TLR7 激动剂
GS-9620是Toll样受体7的有效选择性口服活性小分子激动剂。
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- Yu-Geun Ji, .et al. Determination of motolimod concentration in rat plasma by liquid chromatography-tandem mass spectrometry and its application in a pharmacokinetic study, J Pharm Biomed Anal, 2019, 12 November, 112987
- Zhikuan Zhang, .et al. Structural Analyses of Toll-like Receptor 7 Reveal Detailed RNA Sequence Specificity and Recognition Mechanism of Agonistic Ligands, Cell Reports, 2018, 25(12): 3371-3381.e5 PMID: 30566863
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TLR4 抑制剂
TAK-242的S对映体。TAK-242(Resatorvid),Toll样受体(TLR)4信号转导的小分子抑制剂。TAK-242用于治疗败血症和败血性休克。
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TLR7 激动剂
Isatoribine是一种新型的鸟苷类似物,在体内和体外均显示出免疫刺激活性。
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TLR7/8 激动剂
Resiquimod是一种免疫应答调节剂,可作为有效的TLR 7/8激动剂。阶段2。
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TLR4 antagonist
IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein.
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MD2-TLR4 inhibitor
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
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TLR7 agonist
PF-4878691 (3M-852A) is a potent, orally active, and selective Toll-like receptor 7 (TLR7) agonist modelled to dissociate its antiviral and inflammatory activities.
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TLR4 inhibitor
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases.
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TLR7/8 agonist
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
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TLR inhibitor
AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.
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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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CCR3 拮抗剂
GW 766994 is a specific and oral chemokine receptor-3 (CCR3) antagonist, which has entered clinical trial for asthma and eosinophilic bronchitis.
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CCR8 拮抗剂
AZ084 is a potent, selective, allosteric and oral active CCR8 antagonist, with a Ki of 0.9 nM. Has potential to treat asthma.
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CCR8 抑制剂
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca2+ concentrations.
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CCR4 拮抗剂
CCR4 antagonist 2 (Compound 31) is a novel potent, orally bioavailable small molecule antagonists of CC chemokine receptor 4 (CCR4) that inhibits Treg trafficking into the Tumor Microenvironment without suppressing the number of Treg in healthy tissues.
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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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COX-1 抑制剂
Ibuprofen (Advil)是一种非甾体抗炎药(NSAID),靶向COX-1,IC50为13 μM。
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- 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-1 抑制剂
Ibuprofen Lysine(Motrin)是一种非甾体抗炎药。
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COX-2 抑制剂
Asaraldehyde (Asaronaldehyde)是一种选择性的COX-2抑制剂。
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COX-2 抑制剂
Celecoxib是一种磺胺类非甾体抗炎药(NSAID)和选择性COX-2抑制剂,在Sf9细胞中IC50为40 nM。
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COX 抑制剂
Pravadoline (WIN 48098)是抗炎和前列腺素合成抑制剂,通过抑制环氧合酶(COX)发挥作用。
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- Sharma P, .et al. [3 + 2]-Annulations of N-Hydroxy Allenylamines with Nitrosoarenes: One-Pot Synthesis of Substituted Indole Products, Org Lett, 2016, Feb 5;18(3):412-5 PMID: 26745849
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COX 抑制剂
Sulindac (Clinoril) 是一种非甾体类COX抑制剂,可有效抑制前列腺素的合成。
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COX 抑制剂
Flunixin Meglumin是一种有效的环氧化酶(COX)抑制剂,用作止痛剂,具有抗炎和解热作用。
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- Yukari Nakajima, .et al. Near-Infrared Fluorescence Imaging Directly Visualizes Lymphatic Drainage Pathways and Connections between Superficial and Deep Lymphatic Systems in the Mouse Hindlimb, Sci Rep, 2018, 8: 7078 PMID: 29728629
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COX 抑制剂
Acemetacin (Emflex)是一种非甾体类抗炎药,是吲哚美辛的乙醇酸酯,是一种环加氧酶抑制剂。
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COX-2 抑制剂
Tolfenamic Acid是一种COX-2抑制剂,IC50为0.2μM。它是非甾体抗炎药(NSAID)的一类。它用于治疗偏头痛的症状。
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COX-2 抑制剂
Nimesulide是一种具有镇痛和解热特性的相对COX-2选择性,非甾体抗炎药(NSAID)。
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COX 抑制剂
Lornoxicam (Xefo)是一种非甾体类COX-1/COX-2抑制剂。它是oxicam类的非甾体类抗炎药(NSAID),具有镇痛(缓解疼痛),抗炎和退烧(退烧)特性。
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