CAS:92-61-5
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥98%
Appearance:Light yellow to yellow Solid
Scopoletin 是一种乙酰胆碱酯酶 (AChE) 抑制剂。
Array ( [133] => Array ( [id] => 133 [name] => Inhibitors & Antagonists & Agonists [num] => 3416 [children] => Array ( [352] => Array ( [id] => 352 [name] => Protein Tyrosine Kinase/PTK ) [350] => Array ( [id] => 350 [name] => PI3K/Akt/mTOR ) [351] => Array ( [id] => 351 [name] => Endocrinology & Hormones ) [357] => Array ( [id] => 357 [name] => Angiogenesis ) [358] => Array ( [id] => 358 [name] => HIF ) [363] => Array ( [id] => 363 [name] => Immunology & Inflammation ) [364] => Array ( [id] => 364 [name] => Stem Cells ) [365] => Array ( [id] => 365 [name] => Apoptosis ) [377] => Array ( [id] => 377 [name] => Metabolic Enzyme & Protease ) [379] => Array ( [id] => 379 [name] => Autophagy ) [380] => Array ( [id] => 380 [name] => ER Stress ) [384] => Array ( [id] => 384 [name] => Cell Cycle ) [385] => Array ( [id] => 385 [name] => Cytoskeleton ) [386] => Array ( [id] => 386 [name] => DNA Damage & DNA Repai ) [387] => Array ( [id] => 387 [name] => Epigenetics ) [388] => Array ( [id] => 388 [name] => Ubiquitin ) [389] => Array ( [id] => 389 [name] => JAK/STAT ) [390] => Array ( [id] => 390 [name] => GPCR & G Protein ) [391] => Array ( [id] => 391 [name] => Neuronal Signal Pathway ) [392] => Array ( [id] => 392 [name] => MAPK ) [393] => Array ( [id] => 393 [name] => NF-κB ) [394] => Array ( [id] => 394 [name] => Membrane Transporter & Ion Channel ) [395] => Array ( [id] => 395 [name] => TGF-β/Smad ) [396] => Array ( [id] => 396 [name] => Hippo ) [775] => Array ( [id] => 775 [name] => Antibody-drug Conjugate/ADC Related ) [122] => Array ( [id] => 122 [name] => Others ) ) ) )
>
Small Molecule Compounds >
Inhibitors & Antagonists & Agonists >
Neuronal Signal Pathway >
ScopoletinCAS:92-61-5
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥98%
Appearance:Light yellow to yellow Solid
CAS | 92-61-5 |
Chinese Name | 东莨菪内酯 |
English Name | Scopoletin |
Synonyms | Esculetin 6-methyl ether;Gelseminic acid;6-Methylesculetin;Chrysatropic acid |
Molecular Formula | C10H8O4 |
Molecular Weight | 192.17 |
Solubility | Soluble in DMSO |
Purity | HPLC≥98% |
Appearance | Light yellow to yellow Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 202-171-9 |
MDL | MFCD00006872 |
SMILES | O=C1C=CC2=CC(OC)=C(O)C=C2O1 |
Target Point | AChE |
Passage | Neuronal Signaling |
Background | Scopoletin is an acetylcholinesterase (AChE) inhibitor. |
Biological Activity | Scopoletin 是一种乙酰胆碱酯酶 (AChE) 抑制剂。[1-2] |
In Vitro | Scopoletin(SCT)被鉴定为乙酰胆碱酯酶(AChE)的推定抑制剂。 Scopoletin增强了大鼠额叶皮质突触体中K +刺激的ACh释放,显示出钟形剂量效应曲线(Emax:4μM)[1]。东莨菪碱通过诱导PC3细胞凋亡来抑制PC3增殖。用于抑制PC3,PAA(人肺癌细胞)和Hela细胞增殖的Scopoletin的IC50分别为(157±25),(154±51)和(294±100)mg/L.东莨菪素诱导显著的时间和浓度依赖性抑制PC3细胞增殖。东莨菪素以浓度依赖性方式降低蛋白质含量并降低PC3细胞中的酸性磷酸酶活性(ACP)水平。用Scopoletin处理的细胞通过光学显微镜,荧光显微镜和透射电子显微镜显示细胞凋亡的典型形态变化。 Scopoletin 0,100,200和400 mg/L的细胞凋亡率分别为0.3%,2.1%,9.3%和35%,用Scopoletin处理后G2期细胞明显减少[2]。 |
In Vivo | 东莨菪素(2μg,icv)增加T迷宫交替并改善东莨菪碱诱导的胆碱能缺乏对小鼠的新物体识别。它还减少了15-18个月大的小鼠(2mg/kg sc)的对象记忆中与年龄相关的缺陷。注射2μgScopoletin的小鼠显示交替率增加71.3±2.5%[1]。 |
Cell Experiment | 将指数生长的1mL PC3细胞(5×107/L)接种到4个24孔板中。将板在37℃下在潮湿的5%CO 2气氛中温育。 24小时后,向孔中加入Scopoletin 33,66,133,266和533mg/L(每个板的每个浓度3个孔)。对于对照细胞(前板3个孔),仅加入DMEM。将板连续孵育。通过台盼蓝染料排除法[4],每天在第4天用血细胞计数器计数活细胞。 |
Animal Experiment | 小鼠[1] C56BL/6N雄性,4-6个月大和16-18个月大的小鼠用于行为研究。在恒定湿度(50-55%)和温度(22±1℃)下,在12:12小时光照/黑暗循环(7:00-19:00h)下将小鼠分成4只一组饲养。食物和水随意。较年轻的小鼠(4-6个月)植入icv套管,用于施用东莨菪碱(SCOP)和东莨菪素。通过sc途径向老年小鼠注射东莨菪素。实验在8:00至16:00之间进行。将具有icv套管的小鼠随机分成四个实验组:载体; SCOP20μg; Scopoletin2μg;和SCOP20μg加Scopoletin2μg。将药物施用于1μL载体溶液(SCOP:盐水,Scopoletin:3DMSO:7无菌水)中。在测试开始前15分钟进行Icv注射。在对象记忆测试前30分钟,老年小鼠获得Scopoletin sc(载体:1 DMSO:1 EtOH,根据需要用橄榄油稀释)[1]。 |
Data Literature Source | [1]. Hornick A,et al. The coumarin Scopoletin potentiates acetylcholine release from synaptosomes,amplifies hippocampal long-term potentiation and ameliorates anticholinergic- and age-impaired memory. Neuroscience. 2011 Dec 1;197:280-92. [2]. Liu XL,et al. Effect of Scopoletin on PC3 cell proliferation and apoptosis. Acta Pharmacol Sin. 2001 Oct;22(10):929-33. |
Unit | Bottle |
Specification | 10mg 10mM*1mL in DMSO 20mg |
Scopoletin 是一种乙酰胆碱酯酶 (AChE) 抑制剂。