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L-Eflornithine (L-DFMO) Sale

(Synonyms: L-依氟鸟氨酸; L-DFMO; L-RMI71782; L-α-difluoromethylornithine) 目录号 : GC33414

L-依氟鸟氨酸 (L-DFMO) (L-DFMO) 是依氟鸟氨酸的对映异构体。 L-依氟鸟氨酸 (L-DFMO) 是一种不可逆的鸟氨酸脱羧酶 (ODC) 抑制剂,KD 为 1.3῱0.3 μM,Kinact 为 0.15±0.03 min-1。

L-Eflornithine (L-DFMO) Chemical Structure

Cas No.:66640-93-5

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5mg
¥982.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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].

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]. The L-Eflornithine also appears to be more potent in cultured T.brucei gambiense parasites[2].

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].

[1]. Qu N, et al. Inhibition of human ornithine decarboxylase activity by enantiomers of difluoromethylornithine. Biochem J. 2003 Oct 15;375(Pt 2):465-70. [2]. Jansson-L?fmark R, et al. Enantiospecific reassessment of the pharmacokinetics and pharmacodynamics of oral eflornithine against late-stage Trypanosoma brucei gambiense sleeping sickness. Antimicrob Agents Chemother. 2015 Feb;59(2):1299-307.

Chemical Properties

Cas No. 66640-93-5 SDF
别名 L-依氟鸟氨酸; L-DFMO; L-RMI71782; L-α-difluoromethylornithine
Canonical SMILES N[C@](CCCN)(C(F)F)C(O)=O
分子式 C6H12F2N2O2 分子量 182.17
溶解度 Soluble in DMSO 储存条件 Store at -20°C
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1 mM 5.4894 mL 27.4469 mL 54.8938 mL
5 mM 1.0979 mL 5.4894 mL 10.9788 mL
10 mM 0.5489 mL 2.7447 mL 5.4894 mL
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