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2-氨基二环[2.2.1]庚烷-2-羧酸

2-氨基二环[2.2.1]庚烷-2-羧酸用途

LAT1-IN-1 (BCH) 是 L 型氨基酸转运蛋白 1 (LAT1) 的选择性竞争性抑制剂,可显著抑制细胞对氨基酸的摄取和 mTOR 磷酸化,从而抑制癌细胞生长并诱导细胞凋亡。

2-氨基二环[2.2.1]庚烷-2-羧酸名称

[ CAS 号 ]:
20448-79-7

[ 中文名 ]:
2-氨基-2-去甲菠烷羧酸

[ 英文名 ]:
BCH

[中文别名 ]:

2-氨基-2-降莰烷羧酸

[英文别名 ]:

2-aminonorbornane-2-carboxylic acid
MFCD00167580
b-BCH
2-AMINO-2-NORBORNANE-CARBOXYLIC ACID

2-氨基二环[2.2.1]庚烷-2-羧酸生物活性

[ 描述 ]:

LAT1-IN-1 (BCH) 是 L 型氨基酸转运蛋白 1 (LAT1) 的选择性竞争性抑制剂,可显著抑制细胞对氨基酸的摄取和 mTOR 磷酸化,从而抑制癌细胞生长并诱导细胞凋亡。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

[ 靶点 ]

LAT1[1]

[体外研究]

LAT1-IN-1(1-100 mM；3天；KYSE30和KYSE150食管癌细胞)治疗以剂量依赖性方式抑制细胞增殖[1]。LAT1-IN-1(30 mM；24和48小时；KYSE30和KYSE150细胞)处理显着增加KYSE30和KYSE150细胞中G0/G1期的细胞群,表明LAT1-IN-1诱导细胞周期停滞在G1期[1]。LAT1-IN-1(30mM；0-24小时；KYSE30和KYSE150细胞)处理在30分钟时降低4E-BP1和p70S6K的磷酸化,并持续降低24小时。mTOR,4E-BP1和p70S6K蛋白的含量略有下降[1]。细胞增殖试验[1]细胞系：KYSE30和KYSE150食管癌细胞浓度：1 mM,3 mM,5 mM,10 mM,20 mM,30 mM,40 mM,50 mM或100 mM孵育时间：3天结果：以剂量依赖性方式抑制细胞增殖。细胞周期分析[1]细胞系：KYSE30和KYSE150细胞浓度：30mM孵育时间：24和48小时结果：细胞周期停滞。蛋白质印迹分析[1]细胞系：KYSE30和KYSE150细胞浓度：30mM孵育时间：0小时,0.5小时,1小时,3小时,6小时,24小时结果：4E-BP1和p70S6K的磷酸化降低。mTOR,4E-BP1和p70S6K蛋白的量略微减少。

[体内研究]

LAT1-IN-1(200 mg/kg；静脉注射；每日；14天；雄性BALB/c裸鼠)治疗显着延迟肿瘤生长并降低葡萄糖代谢,表明LAT1抑制可能抑制体内食管癌的生长[1]]。动物模型：雄性BALB/c裸鼠(5周龄),KYSE150细胞[1]剂量：200 mg/kg给药：静脉注射；每日；14天结果：显着延迟肿瘤生长和降低葡萄糖代谢。

[参考文献]

[1]. Ohshima Y, et al. Efficacy of system l amino acid transporter 1 inhibition as a therapeutic target in esophageal squamous cell carcinoma. Cancer Sci. 2016 Oct;107(10):1499-1505.

[2]. Singh N, et al. Discovery of Potent Inhibitors for the Large Neutral Amino Acid Transporter 1 (LAT1) by Structure-Based Methods. Int J Mol Sci. 2018 Dec 21;20(1).

[3]. Wang Q, et al. L-type amino acid transport and cancer: targeting the mTORC1 pathway to inhibit neoplasia. Am J Cancer Res. 2015 Mar 15;5(4):1281-94. eCollection 2015.

2-氨基二环[2.2.1]庚烷-2-羧酸物理化学性质

[ 密度 ]:
1.256g/cm3

[ 沸点 ]:
295.5ºC at 760 mmHg

[ 熔点 ]:
>300 °C(lit.)

[ 分子式 ]:
C₈H₁₃NO₂

[ 分子量 ]:
155.19400

[ 闪点 ]:
132.5ºC

[ 精确质量 ]:
155.09500

[ PSA ]:
63.32000

[ LogP ]:
1.28880

[ 外观性状 ]:
白色至类白色粉末

[ 蒸汽压 ]:
0.000369mmHg at 25°C

[ 折射率 ]:
1.559

[ 储存条件 ]:
室温

2-氨基二环[2.2.1]庚烷-2-羧酸MSDS

详细MSDS(安全技术说明书)

2-氨基二环[2.2.1]庚烷-2-羧酸安全信息

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ 海关编码 ]:
2922499990

2-氨基二环[2.2.1]庚烷-2-羧酸合成路线

详细合成路线

2-氨基二环[2.2.1]庚烷-2-羧酸上下游产品

2-氨基二环[2.2.1]庚烷-2-羧酸上游产品

2-氨基二环[2.2.1]庚烷-2-羧酸下游产品

2-氨基二环[2.2.1]庚烷-2-羧酸海关

[ 海关编码 ]: 2922499990

[ 中文概述 ]:
2922499990 其他氨基酸及其酯及它们的盐（含有一种以上含氧基的除外）. 增值税率:17.0% 退税率:9.0% 监管条件:AB(入境货物通关单,出境货物通关单) 最惠国关税:6.5% 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乙醇胺及其盐应报明色度, 乙醇胺及其盐应报明包装

[ 监管条件 ]: A.入境货物通关单 B.出境货物通关单

[ 检验检疫 ]: P.进境动植物、动植物产品检疫 Q.出境动植物、动植物产品检疫 R.进口食品卫生监督检验 S.出口食品卫生监督检验 M.进口商品检验 N.出口商品检验

[ Summary ]:
HS:2922499990 other amino-acids, other than those containing more than one kind of oxygen function, and their esters; salts thereof VAT:17.0% Tax rebate rate:9.0% Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward) MFN tariff:6.5% General tariff:30.0%

2-氨基二环[2.2.1]庚烷-2-羧酸文献

Dietary methionine can sustain cytosolic redox homeostasis in the mouse liver.

Nat. Commun. 6 , 6479, (2015)

Across phyla, reduced nicotinamide adenine dinucleotide phosphate (NADPH) transfers intracellular reducing power to thioredoxin reductase-1 (TrxR1) and glutathione reductase (GR), thereby supporting f...

Development of a cell-based screening method for compounds that inhibit or are transported by large neutral amino acid transporter 1, a key transporter at the blood-brain barrier.

Anal. Biochem. 486 , 81-5, (2015)

Large neutral amino acid transporter 1 (LAT1) transports neutral amino acids with aromatic or branched side chains as well as their derivatives or prodrugs. Because the transporter is highly expressed...

Effects of gabapentin and pregabalin on K+-evoked 3H-GABA and 3H-glutamate release from human neocortical synaptosomes.

Naunyn Schmiedebergs Arch. Pharmacol. 379(4) , 361-9, (2009)

One site of action of the anticonvulsant, analgesic, and anxiolytic drugs gabapentin and pregabalin is the alpha(2)delta-subunit of voltage-sensitive Ca(2+) channels (VSCC). We therefore analyzed the ...

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