L-依氟鸟氨酸盐酸盐
中文名称 | L-依氟鸟氨酸盐酸盐 |
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中文同义词 | L-依氟鸟氨酸盐酸盐;化合物 T11812L |
英文名称 | L-Eflornithine monohydrochloride |
英文同义词 | L-Eflornithine monohydrochloride;L-DFMO monohydrochloride;L-RMI71782 monohydrochloride;L-α-difluoromethylornithine monohydrochloride;LEflornithine monohydrochloride,L Eflornithine monohydrochloride |
CAS号 | 69955-42-6 |
分子式 | C6H13ClF2N2O2 |
分子量 | 218.63 |
EINECS号 | |
相关类别 | |
Mol文件 | 69955-42-6.mol |
结构式 | ![]() |
L-依氟鸟氨酸盐酸盐 性质
储存条件 | Store at -20°C |
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溶解度 | 溶于二甲基亚砜 |
形态 | 固体 |
颜色 | 浅黄至黄色 |
KD:1.3±0.3 µM (Ornithine decarboxylase, ODC)
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 (K
D
) 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 (K
inact
) 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.
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.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
---|---|---|---|---|---|
2024/04/30 | HY-B0744D | L-Eflornithine monohydrochloride | 5 mg | 968元 | |
2024/04/30 | HY-B0744D | L-依氟鸟氨酸盐酸盐 L-Eflornithine monohydrochloride | 69955-42-6 | 10mg | 1550元 |