消旋型二氟甲基腈盐酸盐
L-依氟鸟氨酸(L-Eflornithine)
CAS: 66640-93-5
化学式: C6H12F2N2O2
| 中文名 | L-依氟鸟氨酸 |
| 英文名 | L-Eflornithine |
| 别名 | L-依氟鸟氨酸 化合物 T11812 消旋型二氟甲基腈盐酸盐 L-ALPHA-二氟甲基鸟氨酸 |
| 英文别名 | DFMO EFLORNITINE L-Eflornithine H-DL-(F2ME)ORN-OH DIFLUOROMETHYLORNITHINE ALPHA-DIFLUORO-ME-DL-ORNITHINE L-alpha-Difluoromethylornithine DL-ALPHA-DIFLUOROMETHYLORNITHINE ALPHA-DIFLUOROMETHYL-DL-ORNITHINE |
| CAS | 66640-93-5 |
| 化学式 | C6H12F2N2O2 |
| 分子量 | 182.17 |
| 密度 | 1.293±0.06 g/cm3(Predicted) |
| 沸点 | 347.0±42.0 °C(Predicted) |
| 酸度系数 | 1.22±0.44(Predicted) |
| 存储条件 | 2-8°C，密封，干燥 |
| 体外研究 | 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. |
| 体内研究 | 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. |
