Powder: -20°C for 3 years | In solvent: -80°C for 1 year
L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 μM, and a Kinact of 0.15±0.03 min-1. L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 663 | 5日内发货 | ||
100 mg | ¥ 5,150 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,420 | 5日内发货 |
产品描述 | L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 μM, and a Kinact of 0.15±0.03 min-1. L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. |
靶点活性 | Ornithine decarboxylase,ODC:(kd)1.3±0.3 µM |
体外活性 | 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.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. |
体内活性 | The typical oral clearances of L-Eflornithine and D-eflornithine are 17.4 and 8.23 liters/h, respectively.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. |
别名 | L-α-difluoromethylornithine monohydrochloride, L-RMI71782 monohydrochloride, L-DFMO monohydrochloride |
分子量 | 218.63 |
分子式 | C6H13ClF2N2O2 |
CAS No. | 69955-42-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
L-Eflornithine monohydrochloride 69955-42-6 Others L-a-difluoromethylornithine Monohydrochloride L-Eflornithine L-RMI-71782 L-RMI71782 Monohydrochloride L-RMI 71782 L-α-difluoromethylornithine monohydrochloride L-RMI-71782 Monohydrochloride L-a-difluoromethylornithine LEflornithine monohydrochloride L-RMI71782 monohydrochloride L-DFMO Monohydrochloride L-RMI71782 L-α-difluoromethylornithine Monohydrochloride L-Eflornithine Monohydrochloride L-RMI 71782 Monohydrochloride L-DFMO monohydrochloride L Eflornithine monohydrochloride L-alpha-difluoromethylornithine Monohydrochloride L-α-difluoromethylornithine L-alpha-difluoromethylornithine L-DFMO Inhibitor inhibitor inhibit