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

S1R agonist 3 is a potent, selective and brain-penetrant 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.

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S1R agonist 3

S1R agonist 3 Chemical Structure

CAS No. : 401501-66-4

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S1R agonist 3 Related Antibodies

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Description

S1R agonist 3 is a potent, selective and brain-penetrant 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)

In Vitro

S1R agonist 3 (Compound 1) (0.01-10000 nM; 120 min) potently binds to S1R in transfected HEK293 cell membranes with a Ki of 1.5 ± 0.5 nM[1].
S1R agonist 3 (0.01-1 μM; 30 min) acts as a potent S1R agonist in overexpressing CHO cells, inducing S1R-BiP dissociation with an EC50 of 160 ± 8 nM[1].

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

S1R agonist 3 Related Antibodies

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).
In Vivo

S1R agonist 3 (Compound 1) optimally prevents hyperlocomotion in wfs1abKO zebrafish larvae without affecting normal locomotion in wild-type larvae[1].
S1R agonist 3 (0.03 mg/kg; i.p.; single dose; 20 minutes post Aβ25-35 injection) potently reverses Aβ25-35 (HY-P0128)-induced learning and memory impairments in mice[1].

MedChemExpress (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.
Molecular Weight

253.77

Formula

C14H20ClNO
CAS No.
SMILES

ClC1=CC=C(C=C1)OCCN2CCC(CC2)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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S1R agonist 3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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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