规格

价格

库存

数量

2 mg

¥ 485

现货

生物活性

产品描述	L-Eflornithine monohydrochloride 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. L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is utilized in enzymology and polyamine biosynthesis research systems to investigate irreversible inhibition kinetics of ornithine decarboxylase, including enzyme inactivation parameters (KD and Kinact) and their relationship to catalytic turnover regulation in cellular metabolic models. L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is further applied in stereochemical and structure–activity relationship studies evaluating enantiomer-dependent enzyme binding and inhibition efficiency in biochemical assay systems.
靶点活性	Ornithine decarboxylase，ODC:1.3±0.3 µM (Kd)
体外活性	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.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.
体内活性	The typical oral clearances of L-Eflornithine and D-eflornithine are 17.4 and 8.23 liters/h, respectively.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.
别名	L-依氟鸟氨酸盐酸盐, L-α-difluoromethylornithine monohydrochloride, L-RMI71782 monohydrochloride, L-DFMO monohydrochloride

化学信息

分子量	218.63
分子式	C₆H₁₃ClF₂N₂O₂
CAS No.	69955-42-6
Smiles	[C@@](CCCN)(C(F)F)(C(O)=O)N.Cl
密度	1.31g/cm3

储存&溶解度

存储

Keep away from moisture, Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

H2O: 40 mg/mL (182.96 mM), Sonication is recommended.

DMSO: 160 mg/mL (731.83 mM), Sonication is recommended.

溶液配制表

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	4.5739 mL	22.8697 mL	45.7394 mL	228.6969 mL
5 mM	0.9148 mL	4.5739 mL	9.1479 mL	45.7394 mL
10 mM	0.4574 mL	2.2870 mL	4.5739 mL	22.8697 mL
20 mM	0.2287 mL	1.1435 mL	2.2870 mL	11.4348 mL
50 mM	0.0915 mL	0.4574 mL	0.9148 mL	4.5739 mL
100 mM	0.0457 mL	0.2287 mL	0.4574 mL	2.2870 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

L-Eflornithine monohydrochloride

L-Eflornithine monohydrochloride

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词