L-DABA(Synonyms: L-2,4-Diaminobutyric acid)

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L-DABA (Synonyms: L-2,4-Diaminobutyric acid)

L-DABA (L-2,4-Diaminobutyric acid)是GABA转氨酶的弱抑制剂,IC50 值大于500 μM。在体内和体外具有抗肿瘤活性。

L-DABA(Synonyms: L-2,4-Diaminobutyric acid)

L-DABA Chemical Structure

CAS No. : 1758-80-1

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生物活性

L-DABA (L-2,4-Diaminobutyric acid) is a week GABA transaminase inhibitor with an IC50 of larger than 500 μM; exhibits antitumor activity in vivo and in vitro.

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(In Vitro)

The tumor cells are irreversibly and totally damaged by incubation with 10 mM L-2,4-Diaminobutyric acid for 24 h at 37°C. The cell-destructive effect by L-DABA is probably due to an osmotic lysis induced by the non-saturated intracellular accumulation of L-DABA. The harmful effect of L-DABA could be abolished by concomitant incubation with L-alanine and L-methionine[1]. Kinetic studies indicates that L-DABA is a non-linear, non-competitive inhibitor of GABA transaminase activity. The L-DABA-induced elevation of GABA levels parallels the inhibition of GABA transaminase activity[2]. L-2,4-Diaminobutyric acid, an amino acid analogue, produceS a cytolytic effect with a human glioma cell line, SKMG-1, and normal human fibroblasts. The concentrations of L-DABA necessary to reduce the cell count to 50% of control following a 24-h incubation at 37°C are 12.5 mM for the human fibroblasts and 20 mM for the glioma cell line[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Treatment with L-DABA results in 43.4% reduction of tumor growth[1]. L-DABA is a more effective inhibitor of GABA transaminase in vivo than in vitro[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

118.13

Formula

C4H10N2O2

CAS 号

1758-80-1

中文名称

L-2,4-二氨基丁酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

H2O : 1 mg/mL (8.47 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 8.4653 mL 42.3263 mL 84.6525 mL
5 mM 1.6931 mL 8.4653 mL 16.9305 mL
10 mM

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Ronquist G, et al. Antitumor activity of L-2,4 diaminobuturic acid against mouse fibrosarcoma cells in vitro and in vivo. J Cancer Res Clin Oncol. 1980;96(3):259-68.

    [2]. Beart PM, et al. l-2,4-Diaminobutyric acid and the GABA system. Neurosci Lett. 1977 Jul;5(3-4):193-8.

    [3]. Panasci L, et al. The cytolytic effect of L-2,4 diaminobutyric acid with malignant glioma cells and fibroblasts. Cancer Chemother Pharmacol. 1988;21(2):143-4.

Animal Administration
[2]

Mice: Male Sprague Dawley rats (150-200g) are used in the study. LDABA is dissolved in 09.% saline and diluted in appropriate medium. L-DABA is administered intraperitoneally at a dose of 764 mg/kg in a volume of 4 mL/kg in acute studies. Chronically treated rats receives daily intraperitoneally injections (2.5mM/kg in saline) for 3 days. Mice are sacrificed and the brain regions are dissected for analysis[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Ronquist G, et al. Antitumor activity of L-2,4 diaminobuturic acid against mouse fibrosarcoma cells in vitro and in vivo. J Cancer Res Clin Oncol. 1980;96(3):259-68.

    [2]. Beart PM, et al. l-2,4-Diaminobutyric acid and the GABA system. Neurosci Lett. 1977 Jul;5(3-4):193-8.

    [3]. Panasci L, et al. The cytolytic effect of L-2,4 diaminobutyric acid with malignant glioma cells and fibroblasts. Cancer Chemother Pharmacol. 1988;21(2):143-4.

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