L-RMI71782 monohydrochloride
L-Eflornithine monohydrochloride
CAS: 69955-42-6
Molecular Formula: C6H13ClF2N2O2
L-RMI71782 monohydrochloride - Names and Identifiers
| Name | L-Eflornithine monohydrochloride |
| Synonyms | L-DFMO monohydrochloride L-RMI71782 monohydrochloride L-Eflornithine monohydrochloride L-α-difluoromethylornithine monohydrochloride |
| CAS | 69955-42-6 |
L-RMI71782 monohydrochloride - Physico-chemical Properties
| Molecular Formula | C6H13ClF2N2O2 |
| Molar Mass | 218.63 |
| Appearance | Solid |
| Storage Condition | 2-8°C，密封，干燥 |
| In vitro study | 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. |
| In vivo study | 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. |
L-RMI71782 monohydrochloride - Reference Information
| biological activity | L-Eflornithine monohydro-chloride (L-DFMO monohydro-chloride) is the enantiomer of eflornitene. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 μm and Kinact of 0.15±0.03 min-1. |
| Target | KD:1.3±0.3 µm (ODC) |
Last Update：2024-04-09 21:11:58
