L-Eflornithine monohydrochloride

L-乙氟鸟氨酸盐酸盐

L-Eflornithine monohydrochloride

L654990-1ml

1ml

10mM in DMSO

干燥,-80℃储存

超低温冰袋运输

L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase ( ODC ) inhibitor with a K D of 1.3±0.3 µM, and a K inact of 0.15±0.03 min -1 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 (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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:KD:1.3±0.3 µM (Ornithine decarboxylase, ODC)

L-氟鸟氨酸单盐酸盐（L-DFMO monohydrochloride）是氟鸟氨酸的对映体。L-flornithine 是一种不可逆的鸟氨酸脱羧酶（ODC）抑制剂，其 K D 为 1.3±0.3 µM，K inact 为 0.15±0.03 min -1 。

69955-42-6(DMSO)

C6H13ClF2N2O2

218.63 g/mol

N[C@](CCCN)(C(F)F)C(O)=O.Cl