Immunology & Inflammation
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GPR3 激动剂/NOS/ NADPH oxidases 抑制剂
Diphenyleneiodonium是一种有效的不可逆的巨噬细胞抑制剂NOS2(iNOS)和内皮细胞NOS3(eNOS)抑制剂。
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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。
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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.
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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.
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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.
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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.
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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。
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- 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
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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)
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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。
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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。
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- 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
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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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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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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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TLR7/8 agonist
TLR7/8 agonist 1 dihydrochloride is a toll-like receptor (TLR7)/TLR8 dual-agonistic imidazoquinoline.
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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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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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