S1R agonist 2

• 常用名: S1R agonist 2
• 英文名: S1R agonist 2
• CAS号: 150085-21-5
• 分子量: 309.45
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₁H₂₇NO
• 熔点: N/A
• 闪点: N/A

S1R agonist 2用途

S1R激动剂2(化合物8b)是选择性S1R激动物,其对于S1R和S2R分别具有1.1nM和88nM的Kis。S1R激动剂2对ROS和NMDA诱导的神经毒性具有神经保护作用[1]。

S1R agonist 2名称

• 英文名: S1R agonist 2

S1R agonist 2生物活性

• 描述: S1R激动剂2(化合物8b)是选择性S1R激动物,其对于S1R和S2R分别具有1.1nM和88nM的Kis。S1R激动剂2对ROS和NMDA诱导的神经毒性具有神经保护作用[1]。
• 相关类别:
  研究领域 >> 神经疾病
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> Sigma Receptor
• 靶点实验:

  Sigma 1 Receptor:1.1 nM (Ki)

  Sigma 2 Receptor:88 nM (Ki)

• 体外研究: S1R激动剂2(化合物8b；0.1-5μM)均能显著增加神经生长因子 (NGF)诱导的神经突生长,且呈剂量依赖性[1] S1R激动剂2(24小时)在 shsy5年细胞中浓度为 1微米时对 鱼藤酮(HY-B1756)诱导的细胞损伤有显著的抑制作用[1] S1R激动剂2(0.1-5μM；24小时)在 shsy5年细胞中对 纳米da刺激有神经保护作用[1] S1R激动剂2(0-10μM；24-72小时)对 A549、罗沃和 Panc-1型细胞无细胞毒性[1]
• 体内研究: S1R激动剂2(化合物8b；0.1-50μM；120小时)在 10微米浓度下不诱导胚胎死亡 (100%存活胚胎),但在最高剂量 (50微米)下诱导所有胚胎死亡[1]
• 参考文献:

  [1]. Linciano P, et al. Novel S1R agonists counteracting NMDA excitotoxicity and oxidative stress: A step forward in the discovery of neuroprotective agents. Eur J Med Chem. 2023 Mar 5;249:115163.

S1R agonist 2物理化学性质

• 分子式: C₂₁H₂₇NO
• 分子量: 309.45
• InChIKey: KOYQYIAABUPJFF-UHFFFAOYSA-N
• SMILES: c1ccc(CC2CCN(CCCOc3ccccc3)CC2)cc1

S1R agonist 2靶点实验

查看更多实验

实验名称：Cytotoxicity against rat PC12 cells assessed as reduction in cell viability at <5 uM ... 来源：ChEMBL 靶标：PC-12 External Id：CHEMBL5333711

实验名称：Selectivity index, ratio of Ki for displacement of [3H]DTG from sigma 2 receptor (unk... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5333709

实验名称：Displacement of [3H]-(+)-pentazocine from sigma 1 receptor (unknown origin) at 25 nM ... 来源：ChEMBL 靶标：Sigma non-opioid intracellular receptor 1 External Id：CHEMBL5333705

实验名称：Displacement of [3H]CGP39653 from human NMDAR at 25 nM by scintillation counting anal... 来源：ChEMBL 靶标：Glutamate receptor ionotropic, NMDA 2C External Id：CHEMBL5333706

实验名称：Toxicity in Zebrafish embryos assessed as variation in embryo morphology score at 1 u... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5333747

实验名称：Toxicity in Zebrafish embryos assessed as variation in embryo morphology score at 10 ... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5333748

实验名称：Toxicity in Zebrafish embryos assessed as death at 50 uM incubated for 5 days by Tera... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5333746

实验名称：Toxicity in Zebrafish embryos assessed as morphological abnormality by observing shor... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5333741

实验名称：Toxicity in Zebrafish embryos assessed as morphological abnormality by observing enla... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5333742

实验名称：Toxicity in Zebrafish embryos assessed as increase in embryo vitality structure damag... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5333739

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