150085-21-5

150085-21-5 structure
150085-21-5 structure
  • Name: S1R agonist 2
  • Chemical Name: S1R agonist 2
  • CAS Number: 150085-21-5
  • Molecular Formula: C21H27NO
  • Molecular Weight: 309.45
  • Catalog: Signaling Pathways GPCR/G Protein Sigma Receptor
  • Create Date: 2023-05-31 19:11:35
  • Modify Date: 2024-01-20 17:31:30
  • S1R agonist 2 (Compound 8b) is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].

Name S1R agonist 2
Description S1R agonist 2 (Compound 8b) is a selective S1R agonist with Kis of 1.1 nM and 88 nM for S1R and S2R, respectively. S1R agonist 2 exhibits neuroprotection against ROS and NMDA-induced neurotoxicity[1].
Related Catalog
Target

Sigma 1 Receptor:1.1 nM (Ki)

Sigma 2 Receptor:88 nM (Ki)

In Vitro S1R agonist 2 (Compound 8b; 0.1-5 μM) 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 agonist 2 (24 h) 在 SHSY5Y 细胞中浓度为 1 μM 时对 Rotenone (HY-B1756) 诱导的细胞损伤有显著的抑制作用[1]。 S1R agonist 2 (0.1-5 μM; 24 h) 在 SHSY5Y 细胞中对 NMDA 刺激有神经保护作用[1]。 S1R agonist 2 (0-10 μM; 24-72 h) 对 A549、LoVo 和 Panc-1 细胞无细胞毒性[1]。
In Vivo S1R agonist 2 (Compound 8b; 0.1-50 μM; 120 h) 在 10 μM 浓度下不诱导胚胎死亡 (100%存活胚胎),但在最高剂量 (50 μM) 下诱导所有胚胎死亡[1]。
References

[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.  

Molecular Formula C21H27NO
Molecular Weight 309.45