西拉美新

• 常用名: 西拉美新
• 英文名: siramesine
• CAS号: 147817-50-3
• 分子量: 454.578
• 密度: 1.2±0.1 g/cm3
• 沸点: 611.4±55.0 °C at 760 mmHg
• 分子式: C₃₀H₃₁FN₂O
• 熔点: N/A
• 闪点: 323.6±31.5 °C

西拉美新用途

Siramesine(Lu 28-179)是sigma-2受体激动剂,能引发癌细胞的死亡,并在体内具有抗癌活性。

西拉美新名称

• 中文名: 西拉美新
• 英文名: 1'-[4-[1-(4-fluorophenyl)indol-3-yl]butyl]spiro[1H-2-benzofuran-3,4'-piperidine]

西拉美新生物活性

• 描述: Siramesine(Lu 28-179)是sigma-2受体激动剂,能引发癌细胞的死亡,并在体内具有抗癌活性。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> Sigma Receptor
  研究领域 >> 癌症
• 参考文献:

  [1]. Cesen MH, et al. Siramesine triggers cell death through destabilisation of mitochondria, but not lysosomes. Cell Death Dis. 2013 Oct 3;4:e818.

  [2]. Spirkoski J, et al. Mast cell apoptosis induced by siramesine, a sigma-2 receptor agonist. Biochem Pharmacol. 2012 Dec 15;84(12):1671-80.

  [3]. Skuza G, et al. The synergistic effect of selective sigma receptor agonists and uncompetitive NMDA receptor antagonists in the forced swim test in rats. J Physiol Pharmacol. 2006 Jun;57(2):217-29.

西拉美新物理化学性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 611.4±55.0 °C at 760 mmHg
• 分子式: C₃₀H₃₁FN₂O
• 分子量: 454.578
• 闪点: 323.6±31.5 °C
• 精确质量: 454.242035
• PSA: 17.40000
• LogP: 9.19
• InChIKey: XWAONOGAGZNUSF-UHFFFAOYSA-N
• SMILES: Fc1ccc(-n2cc(CCCCN3CCC4(CC3)OCc3ccccc34)c3ccccc32)cc1
• 外观性状: 白色固体
• 蒸汽压: 0.0±1.8 mmHg at 25°C
• 折射率: 1.629
• 储存条件: -20℃

西拉美新安全信息

• 危害码 (欧洲): Xi

西拉美新靶点实验

查看更多实验

实验名称：Cytotoxicity against human SH-SY5Y cells at 50 uM after 48 hrs by MTT assay 来源：ChEMBL 靶标：SH-SY5Y External Id：CHEMBL4266802

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：Lipophilicity, log P of the compound 来源：ChEMBL 靶标：N/A External Id：CHEMBL3271176

实验名称：Displacement of [3H]DTG from sigma 2 receptor in Wistar Han rat liver membrane assess... 来源：ChEMBL 靶标：Sigma intracellular receptor 2 External Id：CHEMBL5251999

实验名称：Selectivity ratio of Ki for sigma-1 receptor (unknown origin) to Ki for sigma-2 recep... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3266804

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Binding affinity to sigma2 receptor (unknown origin) assessed as inhibition constant 来源：ChEMBL 靶标：Sigma intracellular receptor 2 External Id：CHEMBL5324497

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

实验名称：Cytotoxicity against human PANC1 cells at 50 uM after 48 hrs by MTT assay 来源：ChEMBL 靶标：PANC-1 External Id：CHEMBL4266810

实验名称：Displacement of [3H](+)-pentazocine from sigma 1 receptor in guinea pig brain membran... 来源：ChEMBL 靶标：Sigma non-opioid intracellular receptor 1 External Id：CHEMBL5251998

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西拉美新英文别名

• QCR-66
• UNII-3IX8CWR24V
• 1'-{4-[1-(4-Fluorophenyl)-1H-indol-3-yl]butyl}-3H-spiro[2-benzofuran-1,4'-piperidine]
• siramesine
• Lu 28-179