|2-氨基二环[2.2.1]庚烷-2-羧酸|CsnPharm

CAS No.: 20448-79-7

BCH Catalog No. CSN22710

Synonyms: BCH;2-Aminobicyclo[2.2.1]heptane-2-carboxylic acid;2-amino-2-Norbornanecarboxylic Acid

BCH is an inhibitor of L-type amino acid transporter LAT1.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述L-Type amino acid transporter 1 (LAT1) is overexpressed in malignant tumor cells to support their growth and proliferation. BCH is a LAT1 inhibitor that inhibits the uptake of [¹⁴C]L-leucine (1μM) in KB, Saos2, and C6 cells with IC50 values of 75.3±6.7μM, 78.8±3.5μM, and 73.1±4.5μM, respectively. BCH also exhibited anti-proliferative effects on KB, Saos2, and C6 cells with IC50 values of 6.9±0.4mM, 5.6±0.7mM, and 6.5 ± 0.9mM, respectively. Treatment of cancer cells with 20 mM BCH significantly increased the proportion of TUNEL-positive cells in comparison to the untreated groups. BCH treatment also significantly promoted proteolytic cleavage of procaspase-7 and procaspase-3 in cancer cells.^[1] Treatment of primary mouse hepatocytes with 10mM BCH led to 38% and 50% increase in cellular and extracellular levels of glutamate, respectively. In normal C57BL/6J mice, treatment with 0.7g/kg BCH for 6 hr significantly increased glutamate level, glutamate dehydrogenase activity, and NAD+/NADH ratio in the liver. In mice fed with high fat/high fructose western diet, peritoneal injection of BCH (0.7g/kg/day) for 8 weeks reduced the level of triglyceride by 30% compared to the control group. BCH treatment also reduced high fat/high fructose diet-induced stress, inflammation and ameliorated hepatic injury and hyperglycemia in mice.^[2]
作用机制BCH is a selective LAT1 inhibitor that can suppress cell growth and induce apoptosis.^[1]
参考文献

[1] Kim CS, Cho SH, Chun HS, Lee SY, Endou H, Kanai Y, Kim DK. BCH, an inhibitor of system L amino acid transporters, induces apoptosis in cancer cells. Biol Pharm Bull. 2008 Jun;31(6):1096-100. doi: 10.1248/bpb.31.1096
[2] Han SJ, Choi SE, Yi SA, Jung JG, Jung IR, Shin M, Kang S, Oh H, Kim HJ, Kim DJ, Kwon JE, Choi CS, Lee KW, Kang Y. Glutamate dehydrogenase activator BCH stimulating reductive amination prevents high fat/high fructose diet-induced steatohepatitis and hyperglycemia in C57BL/6J mice. Sci Rep. 2016 Nov 22;5:37468. doi: 10.1038/srep37468

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 6.4435 mL
- 32.2177 mL
- 64.4354 mL
- 5 mM
- 1.2887 mL
- 6.4435 mL
- 12.8871 mL
- 10 mM
- 0.6444 mL
- 3.2218 mL
- 6.4435 mL

技术信息

CAS号

20448-79-7

储存条件

粉末: Keep in dark place,Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C8H13NO2

运输

蓝冰

分子量

155.19

别名

BCH;2-Aminobicyclo[2.2.1]heptane-2-carboxylic acid;2-amino-2-Norbornanecarboxylic Acid

溶解度

DMSO	1.0 mg/mL (6.4 mM)
Water	30.0 mg/mL (193.3 mM)
Ethanol	Insoluble

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