L-依氟鸟氨酸盐酸盐
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- CAS号:
- 69955-42-6
- 英文名:
- L-Eflornithine monohydrochloride
- 英文别名:
- L-DFMO monohydrochloride;L-RMI71782 monohydrochloride;L-Eflornithine monohydrochloride;L-α-difluoromethylornithine monohydrochloride;LEflornithine monohydrochloride,L Eflornithine monohydrochloride
- 中文名:
- L-依氟鸟氨酸盐酸盐
- 中文别名:
- L-依氟鸟氨酸盐酸盐;化合物 T11812L
- CBNumber:
- CB95419767
- 分子式:
- C6H13ClF2N2O2
- 分子量:
- 218.63
- MOL File:
- 69955-42-6.mol
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L-依氟鸟氨酸盐酸盐化学性质
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储存条件:
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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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形态:
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Solid
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颜色:
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Light yellow to yellow
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L-依氟鸟氨酸盐酸盐性质、用途与生产工艺
L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) 是 Eflornithine 的对映异构体。L-Eflornithine 是一种不可逆的鸟氨酸脱羧酶 (ornithine decarboxylase, ODC) 抑制剂,KD 为 1.3±0.3 μM,Kinact 为 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.
L-依氟鸟氨酸盐酸盐
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更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-B0744D | L-Eflornithine monohydrochloride | | 5 mg | 968元 |
2024/04/30 | HY-B0744D | L-依氟鸟氨酸盐酸盐 L-Eflornithine monohydrochloride | 69955-42-6 | 10mg | 1550元 |
69955-42-6, L-依氟鸟氨酸盐酸盐 相关搜索:
- 化合物 T11812L
- L-依氟鸟氨酸盐酸盐
- 69955-42-6
- LEflornithine monohydrochloride,L Eflornithine monohydrochloride
- L-α-difluoromethylornithine monohydrochloride
- L-RMI71782 monohydrochloride
- L-DFMO monohydrochloride
- L-Eflornithine monohydrochloride