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DL-TBOA ammonium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
DL-TBOA ammonium图片
CAS NO:2093503-71-8

DL-TBOA ammonium 是一种有效的不可运输的兴奋性氨基酸转运蛋白抑制剂,对兴奋性氨基酸转运蛋白 1 (EAAT1),EAAT2EAAT3IC50值分别为 70 μM,6 μM 和 6 μM。DL-TBOA ammonium 抑制表达人EAAT1EAAT2的 COS-1 细胞摄取 [14C]谷氨酸,Ki值分别为 42 μM 和 5.7 μM。DL-TBOA ammonium 以竞争性方式阻断EAAT4EAAT5Ki值分别为 4.4 μM 和 3.2 μM。
生物活性

DL-TBOA ammonium is a potent non-transportable inhibitor ofexcitatory amino acid transporterswithIC50s of 70 μM, 6 μM and 6 μM forexcitatory amino acid transporter-1 (EAAT1),EAAT2andEAAT3, respectively. DL-TBOA ammonium inhibits the uptake of [14C]glutamate in COS-1 cells expressing the humanEAAT1andEAAT2withKivaluesof 42 μM and 5.7 μM, respectively. DL-TBOA ammonium blocksEAAT4andEAAT5in a competitive manner withKivalues of 4.4 μM and 3.2 μM, respectively[1][2][3].

IC50& Target

IC50: 70 μM (EAAT1), 6 μM (EAAT2), 6 μM (EAAT3); Ki: 42 μM (human EAAT1), 5.7 μM (human EAAT2), 4.4 μM (EAAT4), 3.2 μM (EAAT5)[1][2][3]

体外研究
(In Vitro)

DL-TBOA ammonium (70-350 μM; 48 hours) treatment concentration-dependently enhances SN38-induced loss of viability. DL-TBOA reversed Oxaliplatin-induced loss of viability[4].
DL-TBOA ammonium (350 μM; 24 hours) decreases p53 induction by SN38 and oxaliplatin[4].

Cell Viability Assay[4]

Cell Line:HCT116 cells, LoVo cells
Concentration:70 μM, 350 μM
Incubation Time:48 hours
Result:Enhanced SN38-induced, and counteracted Oxaliplatin-induced, cell death.

Cell Viability Assay[4]

Cell Line:HCT116 cells, LoVo cells
Concentration:350 μM
Incubation Time:24 hours
Result:Decreased p53 induction by SN38 and oxaliplatin.
体内研究
(In Vivo)

DL-TBOA ammonium (10 nmol; i.c.v.) to morphine-dependent rats significantly facilitates the expression of naloxone-precipitated somatic signs and conditioned place aversion[5].

Animal Model:Male Sprague-Dawley rats (180-250 g)[5]
Dosage:1 nmol, 3 nmol, 10 nmol
Administration:Intracerebroventricularly injection (i.c.v.)
Result:Dose dependently facilitated various somatic signs induced by Naloxone (0.1 mg/kg)-precipitated morphine withdrawal.
分子量

256.26

Formula

C11H16N2O5

CAS 号

2093503-71-8

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.

 
 
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