2. Neuronal Signaling
  3. Sigma Receptor
  4. S1R agonist 3

S1R agonist 3 是一种强效且选择性的 sigma-1 受体 (S1R) 激动剂，其 Ki 为 1.5 nM。S1R agonist 3 可降低 wfs1abKO 斑马鱼幼体的过度运动行为，且不影响野生型 wfs1abWT 斑马鱼幼体的运动能力。S1R agonist 3 可逆转 Aβ25-35 (HY-P0128) 诱导的学习记忆损伤。S1R ligand 1 可用于阿尔茨海默病的相关研究。

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S1R agonist 3

S1R agonist 3 Chemical Structure

CAS No. : 401501-66-4

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S1R agonist 3 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

S1R agonist 3 is a potent and selective sigma-1 receptor (S1R) agonist with a Ki of 1.5 nM. S1R agonist 3 reduces hyperlocomotion in wfs1abKO zebrafish larvae without affecting locomotion in wildtype wfs1abWT zebrafish larvae. S1R agonist 3 reverses Aβ25-35 (HY-P0128)-induced learning and memory impairments. S1R ligand 1 can be used for the research of Alzheimer’s disease[1].

IC50 & Target[1]

Sigma 1 Receptor

1.5 nM (Ki)

体外研究
(In Vitro)

S1R agonist 3 (Compound 1) (0.01-10000 nM; 120 min) 可强效结合转染 HEK293 细胞膜上的 S1R，其 Ki 值为 1.5 ± 0.5 nM[1]。
S1R agonist 3 (0.01-1 μM; 30 min) 是过表达 CHO 细胞中一种强效的 S1R 激动剂，可诱导 S1R-BiP 解离，其 EC50 为 160 ± 8 nM[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

S1R agonist 3 相关抗体:

ELISA Assay[1]

Cell Line: green fluorescent protein (GFP)-tagged S1R-overexpressing Chinese hamster ovarian (CHO) cells
Concentration: 0.01-1 μM
Incubation Time: 30 min
Result: Induced dissociation of S1R from BiP with an EC50 value of 160 ± 8 nM.
Was blocked by co-treatment with 10 μM S1R antagonist NE-100 (HY-101484A).
体内研究
(In Vivo)

S1R agonist 3 (Compound 1) (3 μM; 24 h) 可在不影响野生型斑马鱼幼体正常运动的前提下，以最优效果抑制 wfs1abKO 斑马鱼幼体的运动过度[1]。
S1R agonist 3 (0.03 mg/kg；腹腔注射；单剂量；Aβ25-35 注射后 20 分钟) 可强效逆转小鼠中由 Aβ25-35 (HY-P0128) 诱导的学习与记忆障碍[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: wfs1abKO mutant larvae; wfs1abWT wild-type larvae (4 days post fertilization)[1]
Dosage: 3 μM
Administration: Continuous exposure in embryo medium; 24 hours
Result: Significantly reduced hyperlocomotion in wfs1abKO larvae, restoring locomotor behavior to levels comparable to wfs1abWT larvae.
Had no significant effect on locomotion in wfs1abWT larvae, resulting in a protection index (PI) within the optimal range of 0.8 < PI < 1.2.
Animal Model: Swiss OF1 (male, 1 month old; intracerebroventricular injection of oligomerized Aβ25-35 peptide)[1]
Dosage: 0.03 mg/kg
Administration: I.p.; single dose; 20 minutes post Aβ25-35 injection
Result: Significantly improved spontaneous alternation performance (a measure of short-term spatial memory) in Aβ25-35-treated mice.
Significantly increased step-through latency (a measure of long-term nonspatial memory) in Aβ25-35-treated mice, reversing Aβ-induced amnesia.
分子量

253.77

Formula

C14H20ClNO
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

S1R agonist 3 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

S1R agonist 3401501-66-4Sigma Receptorwfs1abKO zebrafish larvaeAlzheimer’s diseaseCHO cellsmicesigma-1 receptorwfs1abWT zebrafish larvaehuman S1RHEK293 cell membranesdizocilpinesigma-2 receptorInhibitorinhibitorinhibit

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