MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务。
CAS No. : 1780259-94-0
MCE 国际站:ZK756326 dihydrochloride
产品活性:ZK756326 dihydrochloride 是一种非肽趋化因子受体激动剂,作用于 CC 趋化因子受体 CCR8。
研究领域:GPCR/G Protein | Immunology/Inflammation
作用靶点:CCR
In Vitro: ZK 756326 inhibits the binding of the CCR8 ligand I-309 (CCL1), with an IC50 value of 1.8 μM. ZK 756326 is a full agonist of CCR8, dose-responsively eliciting an increase in intracellular calcium and cross-desensitizing the response of the receptor to CCL1. ZK 756326 stimulates extracellular acidification in cells expressing human CCR8. Binding competition assays are performed on a series of other G-protein-coupled receptors to determine whether the interaction of ZK 756326 is specific for CCR8. In these assays, ZK 756326 is tested at 50 μM for inhibition of radiolabeled ligand binding. At this concentration, ZK 756326 shows >28 fold specificity for CCR8 compared with 26 other GPCRs, all with IC50 values of >50 μM. There is less selectivity when ZK 756326 is tested against the serotonergic receptors 5-HT1A, 5-HT2B, 5-HT2C, 5-HT5A, 5-HT6, and the adrenergic receptor α2A, in which IC50 values of 5.4, 4,4, 34.8, 16, 5.9, and <20 μM (at 20 μM 65% inhibition), respectively, are observed. The compound is unlikely to be an agonist on these biogenic amine receptors, because when tested at concentrations up to 10 μM on a representative receptor, 5-HT1A, it shows no agonist activity in a GTPγS binding assay.
相关产品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Immunology/Inflammation Compound Library | Anti-Cancer Compound Library | Small Molecule Immuno-Oncology Compound Library | Endocrinology Compound Library | Targeted Diversity Library | Chemokine Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Activators Library | DAPTA | BMS-753426 | BMS-813160 | JNJ-27141491 | CCR5 antagonist 2 | AZD-5672 | CCR5 antagonist 3 | Vercirnon | GSK2239633A | Bindarit | Leronlimab | Maraviroc | Plozalizumab | AZD-1678 | CCR4 antagonist 3-1 | Aplaviroc hydrochloride | CCR1 antagonist 6 | J-113863 | CCR1 antagonist 11 hydrochloride | AZD2423 | AZD2098 | RS102895 hydrochloride | LMD-009 | Carlumab | Vicriviroc maleate | CKLF1-C19 | ALK4290 | CCR1 antagonist 10 | INCB 3284 dimesylate
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Fluorescent Dye | PROTAC | Isotope-Labeled Compounds | Oligonucleotides | Antibodies | Click Chemistry
货号: HY-101038A
品牌介绍:
• MCE (MedChemExpress) 拥有200 多种全球独家化合物库,我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物;
• 50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领;
• 产品种类涵盖各种重组蛋白,多肽,常用试剂盒 ,更有 PROTAC、ADC 等特色产品,广泛应用于新药研发、生命科学等科研项目;
• 提供虚拟筛选,离子通道筛选,代谢组学分析检测分析,药物筛选等专业技术服务;
• 设有专业的实验中心和严格的质控、验证体系;
• 提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告,确保产品的高纯度、高品质;
• 产品的生物活性多经各国客户实验验证;
• Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果;
• 专业团队跟踪最新的制药及生命科学研究进展,为您提供全球最新的活性化合物;
• 与世界各大制药公司及知名科研机构建立了长期的合作。