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. : 69955-42-6
MCE 国际站:L-Eflornithine monohydrochloride
产品活性:L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) 是 Eflornithine 的对映异构体。L-Eflornithine 是一种不可逆的鸟氨酸脱羧酶 (ornithine decarboxylase, ODC) 抑制剂,KD 为 1.3±0.3 μM,Kinact 为 0.15±0.03 min-1。
研究领域:Anti-infection
作用靶点:Parasite
In Vitro: Eflornithine (D/L-DFMO) is an inhibitor of ODC, the first enzyme in eukaryotic polyamine biosynthesis. Both enantiomers of Eflornithine (DFMO) irreversibly inactivate ODC. Both Eflornithine enantiomers (L-Eflornithine and D-Eflornithine) suppress ODC activity in a time- and concentration-dependent manner. The inhibitor dissociation constant (KD) values for the formation of enzyme-inhibitor complexes are 28.3±3.4, 1.3±0.3 and 2.2±0.4 µM respectively for D-Eflornithine, L-Eflornithine and Eflornithine. The inhibitor inactivation constants (Kinact) for the irreversible step were 0.25±0.03, 0.15±0.03 and 0.15±0.03 min-1 respectively for D-Eflornithine, L-Eflornithine and Eflornithine. Treatment of human colon tumour-derived HCT116 cells with either L-Eflornithine or D- Eflornithine decreases the cellular polyamine contents in a concentration-dependent manner. The enantiomers display different potencies in vitro, with the L-enantiomer having up to a 20-fold higher affinity for the target enzyme ornithine decarboxylase.
The L-Eflornithine also appears to be more potent in cultured T.brucei gambiense parasites.
In Vivo: The more potent L-Eflornithine is present at much lower concentrations in both plasma and cerebrospinal fluid (CSF) than those of the D-Eflornithine. The plasma concentrations of L-Eflornithine are on average 52% of the D-enantiomer concentrations. The typical oral clearances of L-Eflornithine and D-eflornithine are 17.4 and 8.23 liters/h, respectively.
相关产品:Drug Repurposing Compound Library Plus | FDA-Approved Drug Library Plus | FDA-Approved Drug Library Mini | Bioactive Compound Library Plus | Anti-Infection Compound Library | FDA-Approved Drug Library | Anti-Cancer Compound Library | Drug Repurposing Compound Library | FDA Approved & Pharmacopeial Drug Library | Antiparasitic Compound library | Anti-Cancer Metabolism Compound Library | Targeted Diversity Library | FDA-Approved Anticancer Drug Library | Off-patent Drug Library | Antifungal agent 26 | Quinidine-d3 | Angulatin G | Acridine Orange base | N-Desethyl amodiaquine-d5 | Palitantin | Proguanil-d6 | Azlocillin sodium salt | Methyl palmitate | HBPC–GSH | Doxycycline calcium | SQ109 | 13,21-Dihydroeurycomanone | Nevirapine | Monensin sodium salt | Clindamycin phosphate | 1-Deacetylnimbolinin B | KDU731 | (E)-Fenpyroximate | Niclosamide monohydrate | Antimalarial agent 8 | Geranin A | Cabamiquine | Harpagide | Clopidol | trans-Methylisoeugenol | Morantel tartrate | Berberine | Antileishmanial agent-17
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。