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66640-93-5

中文名稱(chēng) 消旋型二氟甲基腈鹽酸鹽
英文名稱(chēng) DFMO
CAS 66640-93-5
分子式 C6H12F2N2O2
分子量 182.17
MOL 文件 66640-93-5.mol
66640-93-5 結(jié)構(gòu)式 66640-93-5 結(jié)構(gòu)式

基本信息

中文別名
L-依氟鳥(niǎo)氨酸
消旋型二氟甲基腈鹽酸鹽
L-ALPHA-二氟甲基鳥(niǎo)氨酸
英文別名
DFMO
L-DFMO
L-RMI71782
EFLORNITINE
L-Eflornithine
H-DL-(F2ME)ORN-OH
DIFLUOROMETHYLORNITHINE
L-α-difluoromethylornithine
H-ALPHA-DIFLUORO-ME-DL-ORN-OH
ALPHA-DIFLUORO-ME-DL-ORNITHINE

物理化學(xué)性質(zhì)

沸點(diǎn)347.0±42.0 °C(Predicted)
密度1.293±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)1.22±0.44(Predicted)

常見(jiàn)問(wèn)題列表

生物活性
L-Eflornithine (L-DFMO) 是 Eflornithine 的對(duì)映異構(gòu)體。L-Eflornithine 是一種不可逆的鳥(niǎo)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(diǎn)

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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