Immunology & Inflammation
-
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.
了解更多
-
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.
了解更多
-
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.
了解更多
-
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.
了解更多
-
TLR7 激动剂
Imiquimod (Aldara)是一种杂环咪唑并喹啉酰胺，用作免疫反应调节剂。
了解更多
- David Diaz-Carballo, .et al. Enhanced antitumoral activity of TLR7 agonists via activation of human endogenous retroviruses by HDAC inhibitors, Commun Biol, 2021, Mar 3;4(1):276 PMID: 33658617
- Kunishita Y, .et al. TRIM21 Dysfunction Enhances Aberrant B-Cell Differentiation in Autoimmune Pathogenesis, Front Immunol, 2020, Feb 7;11:98 PMID: 32117252
-
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。
了解更多
- 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
-
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。
了解更多
-
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。
了解更多
-
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。
了解更多
-
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.
了解更多
-
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.
了解更多
-
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.
了解更多
-
TLR4 inhibitor
Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor and plays pivotal role in various inflammatory diseases.
了解更多
-
TLR7/8 agonist
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
了解更多
-
TLR inhibitor
AN-3485 is a benzoxaborole analog, Toll-Like Receptor(TLR) inhibitor with IC50 values ranging from 18 to 580 nM.
了解更多
-
TLR7 Ligand
Toll-Like Receptor 7 Ligand II是一种细胞可渗透的羟基腺嘌呤化合物，可作为强效且高度特异性的TLR7（toll样受体7）激动剂，对TLR2/3/5/8/9没有任何可检测的活性。它在刺激体外培养物中产生TLR7依赖性细胞因子方面比R848效力高10倍。
了解更多
-
TLR8 激动剂
VTX-2337是一种具有潜在的免疫刺激和抗肿瘤活性的小分子Toll样受体8（TLR8）激动剂。
了解更多
- Yinwen Cheng, .et al. The anti-tumor effects of cetuximab in combination with VTX-2337 are T cell dependent, Sci Rep, 2021, Jan 15;11(1):1535 PMID: 33452311
-
TLR4 抑制剂
VGX-1027通过抑制Toll样受体4（TLR4）信号传导来显示免疫调节和抗炎活性。
了解更多
-
Hydroxychloroquine Sulfate是一种抗疟疾药，用于治疗系统性红斑狼疮，类风湿性关节炎和其他自身免疫性，炎性和皮肤病性疾病。还可以作为自噬和通行费样受体（TLR）7/9的抑制剂。
了解更多
-
Toll-like receptor modulator是一类在先天免疫系统中起关键作用的蛋白质。是一类在先天免疫系统中起关键作用的蛋白质。
了解更多
-
TLR7 激动剂
Gardiquimod TFA是一种化合物，可选择性作用于小鼠和人类形式的Toll样受体7（TLR7）。它起免疫反应调节剂的作用。CAS：1020412-43-4（游离碱）
了解更多
-
TLR 抑制剂
TLR2-IN-C29是TLR2/1和TLR2/6信号传导的抑制剂。
了解更多
- Qian-Lu Wang, .et al. ROCK1 regulates sepsis-induced acute kidney injury via TLR2-mediated endoplasmic reticulum stress/pyroptosis axis, Mol Immunol, 2021, Oct;138:99-109 PMID: 34365196
-
TLR7 激动剂
TLR7-agonist-1是一种有效且选择性的Toll样受体7（TLR7）激动剂，LEC为0.4 μM。
了解更多
-
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。
了解更多
- 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
-
CXCR4 拮抗剂
AMD 070是CXCR4趋化因子受体拮抗剂。
了解更多
- 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
-
CXCR4 拮抗剂
AMD 3465 Hexahydrobromide是一种有效的选择性CXCR4拮抗剂。
了解更多
- 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
-
CXCR2 ligand
SRT3109是一种CXCR2配体，用于治疗趋化因子介导的疾病和状况。
了解更多
-
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）。
了解更多
-
CXCR4 抑制剂
MSX-122是口服可生物利用的CXCR4抑制剂（IC50 =?10 nM），具有潜在的抗肿瘤和抗病毒活性。CXCR4抑制剂MSX-122与趋化因子受体CXCR4结合，阻止基质衍生因子-1（SDF-1）与CXCR4受体和受体激活结合，这可能导致肿瘤细胞增殖和迁移减少。
了解更多
-
SIRT1 activator
SRT3190是一种强效cxcr2配体。
了解更多
-
CXCL8/CXCR1/2 抑制剂
Reparixin是两种CXCL8受体CXCR1/2的有效抑制剂，它抑制CXCR2介导的细胞迁移（IC50 = 100 nM），而它强烈地阻断CXCR1介导的趋化性（IC50 = 1 nM）。
了解更多
- Naour AL, .et al. Tumor cells educate mesenchymal stromal cells to release chemoprotective and immunomodulatory factors, J Mol Cell Biol, 2019, Sep 3 PMID: 31504643
- Wigenstam E, .et al. N-acetyl cysteine improves the effects of corticosteroids in a mouse model of chlorine-induced acute lung injury, Toxicology, 2015, Feb 3;328:40-7 PMID: 25497111
-
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。
了解更多
- 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
-
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。
了解更多
- 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
-
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。
了解更多
-
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。
了解更多
-
CXCL8 receptor 抑制剂
Reparixin L-lysine salt是CXCL8受体的抑制剂，也抑制CXCR1和CXCR2的活化，已显示在各种损伤模型中减弱了炎症反应。
了解更多
-
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。
了解更多
-
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。
了解更多
-
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。
了解更多
-
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。
了解更多
-
CXCR4 激动剂
ATI-2341是针对C-X-C趋化因子受体4型（CXCR4）（EC50 = 194 nM）的pepducin，是一种变构激动剂，可激活抑制性异三聚体G蛋白（Gi），从而促进cAMP生成的抑制并诱导钙动员。
了解更多
-
CXCR4 receptor modulator
NSC-23026是CXCR4受体调节剂。
了解更多
-
-
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.
了解更多
-
GPR35/CXCR8 拮抗剂
Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
了解更多
-
Human CXCR3 拮抗剂
PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity, which inhibits the binding of CXCR3 ligand CXCL10 to CXCR3 receptor with IC50 of 42 nM.
了解更多
-
CXCR2 激动剂
CXCR2-IN-1 is a central nervous system penetrant CXCR2 antagonists with a pIC50 of 9.3.
了解更多
-
GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
了解更多
-
GPR35/CXCR8 agonist
Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
了解更多
-
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.
了解更多
微信关注
