Immunology & Inflammation
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interleukin-5 receptor 拮抗剂
YM-90709是白介素5受体拮抗剂。YM-90709抑制IL-5与其周围人嗜酸性粒细胞和丁酸处理的嗜酸性HL-60克隆15细胞的受体结合，IC50值分别为1.0和0.57 microM。
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IL-1 receptor 拮抗剂
AF 12198是人I型白介素1（IL-1）受体的有效选择性拮抗剂。
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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 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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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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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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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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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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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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CXCR4 拮抗剂
Plerixafor 8HCl (DB06809)是CXCR4趋化因子受体拮抗剂，作用于CXCR4和CXCL12介导调节的趋化性， IC50分别为44 nM和5.7 nM。
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- Mei Zheng, .et al. CXCL12 inhibits hair growth through CXCR4, Biomed Pharmacother, 2022, Jun;150:112996 PMID: 35462338
- Asiedu KO, .et al. Bone marrow cell homing to sites of acute tibial fracture: 89Zr-oxine cell labeling with positron emission tomographic imaging in a mouse model, EJNMMI Res, 2018, Dec 13;8(1):109 PMID: 30547233
- Kingsley O. Asiedu, .et al. Bone marrow cell trafficking analyzed by 89Zr-oxine positron emission tomography in a murine transplantation model, Clin Cancer Res, 2017, Jun 1; 23(11): 2759-2768 PMID: 27965305
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CXCR4 拮抗剂
AMD 070是CXCR4趋化因子受体拮抗剂。
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- Uchida D, .et al. Effect of a novel orally bioavailable CXCR4 inhibitor, AMD070, on the metastasis of oral cancer cells, Oncol Rep, 2018, Jul;40(1):303-308 PMID: 29749473
- Mamoru Morimoto, .et al. Enhancement of the CXCL12/CXCR4 axis due to acquisition of resistance in pancreatic cancer: effect of CXCR4 antagonists, BMC Cancer, 2016, 16: 305 PMID: 27175473
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CXCR4 拮抗剂
AMD 3465 Hexahydrobromide是一种有效的选择性CXCR4拮抗剂。
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- Kentaro Suzuki, .et al. C-terminal-modifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
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CXCR4 拮抗剂
WZ811是4型C-X-C趋化因子受体（CXCR4）拮抗剂（EC50 = 0.3 nM）。在体外抑制CXCR4/基质细胞衍生因子1（SDF-1）介导的cAMP调节（EC50 = 1.2 nM）。
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CXCR4 拮抗剂
AMD3100 (Plerixafor)是用于增殖造血干细胞的免疫刺激剂，并且是用于动员造血干细胞进行移植的趋化因子受体-4拮抗剂。
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- Hitoshi Maeda, .et al. Cell-penetrating albumin enhances the sublingual delivery of antigens through macropinocytosis, Int J Biol Macromol, 2022, Sep 17;221:1439-1452 PMID: 36126807
- Jingying Chen, .et al. Brain vascular damage-induced lymphatic ingrowth is directed by Cxcl12b/Cxcr4a, Development, 2022, Jul 1;149(13) PMID: 35694896
- Narubhorn Ongprakobkul, .et al. Effects of local vs systemic administration of CXCR4 inhibitor AMD3100 on orthodontic tooth movement in rats, Am J Orthod Dentofacial Orthop, 2022, Mar 2;S0889-5406(22)00107-X PMID: 35248418
- Chunliang Liu, .et al. Positive effects of selenium supplementation on selenoprotein S expression and cytokine status in a murine model of acute liver injury, J Trace Elem Med Biol, 2022, Jan 10;71:126927 PMID: 35030482
- Eri Watanabe, .et al. Stromal cell-derived factor 1 (SDF1) attenuates platelet-derived growth factor-B (PDGF-B)-induced vascular remodeling for adipose tissue expansion in obesity, Angiogenesis, 2020, Jul 22 PMID: 32699964
- Alessandra Esposito, .et al. Role of Prx1-expressing skeletal cells and Prx1-expression in fracture repair, Bone, 2020, Jul 3;139:115521 PMID: 32629173
- Kentaro Suzuki, .et al. C-terminal?Cmodifed LY2510924: a versatile scafold for targeting C-X-C chemokine receptor type 4, Sci Rep, 2019, 9: 15284
- Ichimizu S, .et al. Cell-penetrating mechanism of intracellular targeting albumin: Contribution of macropinocytosis induction and endosomal escape, J Control Release, 2019, May 10;304:156-163 PMID: 31082432
- Nan Li, .et al. LPS-induced CXCR7 expression promotes gastric Cancer proliferation and migration via the TLR4/MD-2 pathway, Diagn Pathol, 2019, Jan 12;14(1):3 PMID: 30636642
- Thida W, .et al. The role of conventional antibodies targeting the CD4 binding site and CD4-induced epitopes in the control of HIV-1 CRF01_AE viruses, Biochem Biophys Res Commun, 2018, Nov 20. pii: S0006-291X(18)32477-X PMID: 30470571
- Henry R. Hampton, .et al. Microbe-dependent lymphatic migration of neutrophils modulates lymphocyte proliferation in lymph nodes, Nat Commun, 2015, 6: 7139 PMID: 25972253
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CXCR1/CXCR2 拮抗剂
SCH-527123 (Navarixin)是人CXCR1和CXCR2受体的强效选择性拮抗剂，IC50分别为42 nM和3 nM。
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- Ruijie Zhang, .et al. Combined inhibition of IL-6 and IL-8 pathways suppresses ovarian cancer cell viability and migration and tumor growth, Int J Oncol, 2022, May;60(5):50 PMID: 35315502
- Fu S, .et al. Inhibition of interleukin 8/C-X-C chemokine receptor 1,/2 signaling reduces malignant features in human pancreatic cancer cells, Int J Oncol, 2018, Jul;53(1):349-357 PMID: 29749433
- Fu S, .et al. Blocking Interleukin-6 and Interleukin-8 Signaling Inhibits Cell Viability, Colony-forming Activity, and Cell Migration in Human Triple-negative Breast Cancer and Pancreatic Cancer Cells, Anticancer Res, 2018, Nov;38(11):6271-6279 PMID: 30396947
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CXCR2 拮抗剂
SB265610是CXCR2 (Kd = 2.51 nM)的非肽变构反向激动剂，通过与不同于激动剂结合位点的区域结合来防止受体活化。它不与相关CXCR1受体结合。在体外和高氧诱导肺损伤的大鼠模型中，它已被证明能防止中性粒细胞趋化性。
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CXCR2 拮抗剂
SB225002是一种有效的选择性CXCR2拮抗剂，IC50为22 nM，可抑制白介素IL-8与CXCR2的结合，选择性是其他测试的7-TMR的150倍以上。
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CXCR2/CXCR1 拮抗剂
SCH 563705是有效的双重CXCR2（IC50 = 1.3 nM)/CXCR1（IC50 = 7.3 nM）拮抗剂。
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CXCR4 拮抗剂
在CXCR4 125I-SDF抑制结合试验中，AMD-070 HCl是一种有效的选择性CXCR4拮抗剂，IC50值为13 nM，抑制T-4型HIV-1（NL4.3株）在MT-4细胞中的复制和PBMC。
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CXCL chemokines 拮抗剂
UNBS5162是一种新型萘二甲酰亚胺，可降低实验性前列腺癌中CXCL趋化因子的表达。9种癌细胞系的平均抗增殖活性IC50值为17.9 uM；UNBS3157的水解产物。
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CXCR2 拮抗剂
AZD-5069是一种有效的选择性CXCR2拮抗剂，具有抑制COPD患者中性粒细胞向气管迁移的潜能。
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CXCR4 拮抗剂
USL311 is a CXCR4 receptor antagonist which prevents the binding of stromal-cell derived factor-1 (SDF-1 or CXCL12) to CXCR4.
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CXCR2 激动剂
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.
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CXCR3 antagonist
AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
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CXCR3 antagonist
SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
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CXCR3 antagonist
AMG 487 S-enantiomer is the S enantiomer of AMG 487. AMG 487 is an antagonist of the chemokine receptor CXCR3.
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CXCR3 antagonist
NBI-74330 is a potent antagonist for CXCR3, and exhibits potent inhibition of (125I)CXCL10 and (125I)CXCL11 specific binding with Ki of 1.5 and 3.2 nM, respectively.
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LTR antagonist
Montelukast (trade name Singulair) is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies.
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LTR antagonist
AS-35 is an orally effective, potent and selective antagonist of leukotrienes, antagonizes LTC4-, LTD4 and LTE4-induced contractions of the ileum with IC50 values of 8 nM, 4 nM and 3 nM, respectively, and has antiallergic activities.
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LTD4 receptor 拮抗剂
MK-0679 (Verlukast)是有效的白三烯D4拮抗剂。
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BLT2 receptors 拮抗剂
LY 255283是一种有效的 BLT2 receptors 拮抗剂。
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CysLT1 receptor 拮抗剂
MK-571是有效的CysLT1（LTD4）白三烯受体反向激动剂，EC50值为1.3 nM。
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- Jung-Hung Chen, .et al. Transplacental transfer of acetaminophen in pregnant rats, Biomed Pharmacother, 2022, Oct;154:113613 PMID: 36058146
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CysLT1 receptor 拮抗剂
MK-571 sodium salt是一种选择性的口服活性CysLT1受体拮抗剂。它阻断LTD4而不是LTC4与人和豚鼠肺膜的结合，Ki值分别为0.22 nM和2.1 nM。
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