DL-TBOA

生物活性靶点体外研究体内研究 DL-TBOA 试剂级价格

DL-TBOA

CAS号:205309-81-5
英文名:DL-TBOA
中文名:DL-TBOA
CBNumber:CB2208679
分子式:C11H13NO5
分子量:239.22
MOL File:Mol file

DL-TBOA化学性质

沸点 :421.7±45.0 °C(Predicted)
密度 :1.392±0.06 g/cm3(Predicted)
储存条件 :Desiccate at -20°C
溶解度 :<23.92mg/ml in DMSO;insoluble in H2O
形态 :solid
酸度系数(pKa) :2.07±0.27(Predicted)
颜色 :White

DL-TBOA性质、用途与生产工艺

生物活性 DL-TBOA 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)，EAAT2 和 EAAT3 的 IC50 值分别为 70 μM，6 μM 和 6 μM。DL-TBOA 抑制表达人 EAAT1 和 EAAT2 的 COS-1 细胞摄取 [14C]谷氨酸，Ki 值分别为 42 μM 和 5.7 μM。DL-TBOA 以竞争性方式阻断 EAAT4 和 EAAT5，Ki 值分别为 4.4 μM 和 3.2 μM。
靶点

IC50: 70 μM (EAAT1), 6 μM (EAAT2) and 6 μM (EAAT3); Ki: 42 μM (human EAAT1), 5.7 μM (human EAAT2), 4.4 μM (EAAT4) and 3.2 μM (EAAT5)

体外研究

DL-TBOA (70-350 μM; 48 hours; HCT116 and LoVo cell lines) treatment concentration-dependently enhances SN38-induced loss of viability. DL-TBOA reversed Oxaliplatin-induced loss of viability.
DL-TBOA (350 μM; 24 hours; HCT116 and LoVo cell lines) treatment decreases p53 induction by SN38 and oxaliplatin.

Cell Viability Assay

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

Cell Viability Assay

Cell Line:	HCT116 and LoVo cell lines
Concentration:	350 μM
Incubation Time:	24 hours
Result:	p53 induction by SN38 and oxaliplatin was decreased.

体内研究

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

Animal Model:	Male Sprague-Dawley rats (180-250 g)
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.