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.
For research use only. We do not sell to patients.
- CAS No.: 401501-66-4
- Formula: C14H20ClNO
- Molecular Weight:253.77
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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Sigma 1 Receptor 1.5 nM (Ki) |
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.
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Cell Line:green fluorescent protein (GFP)-tagged S1R-overexpressing Chinese hamster ovarian (CHO) cells
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Concentration:0.01-1 μM
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Incubation Time:30 min
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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).
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.
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Animal Model:wfs1abKO mutant larvae; wfs1abWT wild-type larvae (4 days post fertilization)[1]
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Dosage:3 μM
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Administration:Continuous exposure in embryo medium; 24 hours
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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.
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Animal Model:Swiss OF1 (male, 1 month old; intracerebroventricular injection of oligomerized Aβ25-35 peptide)[1]
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Dosage:0.03 mg/kg
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Administration:I.p.; single dose; 20 minutes post Aβ25-35 injection
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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.
Chemical Information
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CAS No. 401501-66-4
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Molecular Weight 253.77
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Formula C14H20ClNO
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SMILES
ClC1=CC=C(C=C1)OCCN2CCC(CC2)C
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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