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69955-42-6

中文名稱 L-依氟鳥氨酸鹽酸鹽
英文名稱 L-Eflornithine monohydrochloride
CAS 69955-42-6
分子式 C?H??ClF?N?O?
分子量 218.63
MOL 文件 69955-42-6.mol
69955-42-6 結(jié)構(gòu)式 69955-42-6 結(jié)構(gòu)式

基本信息

中文別名
L-依氟鳥氨酸鹽酸鹽
英文別名
L-DFMO monohydrochloride
L-Eflornithine monohydrochloride

物理化學(xué)性質(zhì)

儲存條件-20°C儲存
溶解度溶于二甲基亞砜
形態(tài)Solid
顏色Light yellow to yellow

常見問題列表

生物活性
L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) 是 Eflornithine 的對映異構(gòu)體。L-Eflornithine 是一種不可逆的鳥氨酸脫羧酶 (ornithine decarboxylase, ODC) 抑制劑,KD 為 1.3±0.3 μM,Kinact 為 0.15±0.03 min-1。
靶點

KD:1.3±0.3 μM (Ornithine decarboxylase, ODC)

體外研究

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.

體內(nèi)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.

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