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. : 356057-34-6
MCE 国际站:Darapladib
产品活性:Darapladib 是一种有效的脂蛋白相关磷脂酶A2 (Lp-PLA2) 抑制剂,IC50 为 0.25 nM。
研究领域:Metabolic Enzyme/Protease
作用靶点:Phospholipase
In Vitro: Mechanistic studies using steady state and transient kinetics indicate Darapladib (SB-480848) to be a freely reversible, non-covalently bound, inhibitor of rhLp-PLA2 with a Ki of 110 pM and an off-rate of 27 min. Potent inhibition of the enzyme in whole human plasma is confirmed (IC50=5±2 nM). Furthermore, the presence of Darapladib during the copper catalysed oxidation of human LDL prevents the production of lyso-PtdCho (IC50=4±3 nM) and subsequent monocyte chemotaxis (IC50=4±1 nM).
In Vivo: Additional in vivo studies with Darapladib indicated an oral bioavailability of 11±2% in the fed rat. The oral bioavailability of Darapladib is 28±4% in the dog. Furthermore excellent inhibition of Lp-PLA2 within the atherosclerotic plaque is achieved for Darapladib, with 95±1% inhibition observed 2 h after an oral dose of 30 mg/kg to the WHHL rabbit. Darapladib, a specific inhibitor of lipoprotein-associated phospholipase A2 (lp-PLA2), on inflammation and atherosclerotic formation in the low density lipoprotein receptor (LDLR)-deficient mice. the activity of serum lp-PLA2 is inhibited by more than 60% in LDLR-deficient mice after oral administration of 50 mg/kg once daily of Darapladib for 6 weeks. Darapladib significantly inhibits serum lp-PLA2 activity in LDLR-deficient mice.
相关产品:Covalent Screening Library Plus | Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Metabolism/Protease Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Covalent Screening Library | Anti-Cardiovascular Disease Compound Library | Anti-COVID-19 Compound Library | Orally Active Compound Library | Lipid Metabolism Compound Library | Targeted Diversity Library | Human Metabolite Library | Sphingomyelin phosphodiesterase | LCL521 dihydrochloride | C12 NBD Sphingomyelin | Cambinol | Neomycin sulfate | D-Erythro-dihydrosphingosine | (R)-Bromoenol lactone | CCT129957 | Melittin | Alminoprofen | ML-298 | MAFP | N-Stearoylsphingomyelin | Aristolochic acid C | Omeprazole-d3-1 | 3-Nitrocoumarin | Pyrrophenone | m-3M3FBS | Tanshinone I | VU 0364739 hydrochloride | Ecopladib | LY 178002 | Varespladib methyl | ML348 | DL-erythro-Dihydrosphingosine | Folipastatin | FKGK18 | LY-311727 | LFHP-1c | Tris(2,4-di-tert-butylphenyl)phosphate
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
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。