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L-Eflornithine (Synonyms: L-依氟鸟氨酸; L-DFMO; L-RMI71782; L-α-difluoromethylornithine)
L-Eflornithine (L-DFMO) 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。
L-Eflornithine Chemical Structure
CAS No. : 66640-93-5
| 规格 | 是否有货 | ||
|---|---|---|---|
| 10 mg | Check price and availability | ||
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L-Eflornithine 的其他形式现货产品:
| 生物活性 |
L-Eflornithine (L-DFMO) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min-1[1]. |
IC50 & Target |
KD:1.3±0.3 µM (Ornithine decarboxylase, ODC)[1] |
|---|---|
| 体外研究 (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 (KD) 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 (Kinact) 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[1]. 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[2]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
| 体内研究 (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[2]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
| 分子量 |
182.17 |
| Formula |
C6H12F2N2O2 |
| CAS 号 |
66640-93-5 |
| 中文名称 |
L-依氟鸟氨酸 |
| 运输条件 |
Room temperature in continental US; may vary elsewhere. |
| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
| 参考文献 |
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