消旋型二氟甲基腈鹽酸鹽
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- CAS號:
- 66640-93-5
- 英文名:
- DFMO
- 英文別名:
- DFMO;L-DFMO;L-RMI71782;EFLORNITINE;L-Eflornithine;H-DL-(F2ME)ORN-OH;DIFLUOROMETHYLORNITHINE;L-α-difluoromethylornithine;L Eflornithine,LEflornithine;H-ALPHA-DIFLUORO-ME-DL-ORN-OH
- 中文名:
- 消旋型二氟甲基腈鹽酸鹽
- 中文別名:
- L-依氟鳥氨酸;化合物 T11812;消旋型二氟甲基腈鹽酸鹽;L-ALPHA-二氟甲基鳥氨酸
- CBNumber:
- CB1373228
- 分子式:
- C6H12F2N2O2
- 分子量:
- 182.17
- MOL File:
- 66640-93-5.mol
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消旋型二氟甲基腈鹽酸鹽化學(xué)性質(zhì)
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沸點(diǎn):
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347.0±42.0 °C(Predicted)
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密度:
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1.293±0.06 g/cm3(Predicted)
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儲存條件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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酸度系數(shù)(pKa):
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1.22±0.44(Predicted)
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消旋型二氟甲基腈鹽酸鹽性質(zhì)、用途與生產(chǎn)工藝
L-Eflornithine (L-DFMO) 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。
KD:1.3±0.3 μM (Ornithine decarboxylase, ODC)
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.
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.
消旋型二氟甲基腈鹽酸鹽
上下游產(chǎn)品信息
上游原料
下游產(chǎn)品
66640-93-5, 消旋型二氟甲基腈鹽酸鹽 相關(guān)搜索:
- 抑制劑
- Angiogenesis Inhibitors
- Cancer Research
- BioChemical
- Angiogenesis
- 化合物 T11812
- L-依氟鳥氨酸
- L-ALPHA-二氟甲基鳥氨酸
- 消旋型二氟甲基腈鹽酸鹽
- 66640-93-5
- L Eflornithine,LEflornithine
- L-DFMO
- L-RMI71782
- L-α-difluoromethylornithine
- L-Ornithine, 2-(difluoromethyl)-
- L-Eflornithine
- H-ALPHA-DIFLUORO-ME-DL-ORN-OH
- H-DL-(ALPHA-DIFLUOROMETHYL)ORN-OH
- H-DL-(F2ME)ORN-OH
- DIFLUOROMETHYLORNITHINE
- DL-ALPHA-DIFLUOROMETHYLORNITHINE
- EFLORNITINE
- DFMO
- L-alpha-Difluoromethylornithine
- ALPHA-DIFLUOROMETHYL-DL-ORNITHINE
- ALPHA-DIFLUORO-ME-DL-ORNITHINE