S1RA

For research use only.

Catalog No.S6754 Synonyms: E-52862

S1RA Chemical Structure

CAS No. 878141-96-9

S1RA (E-52862) is a selective sigma-1 receptor (σ1R) antagonist with a reported binding affinity of Ki = 17.0 ± 7.0 nM for human σ1 receptor , selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels.

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Biological Activity

Description S1RA (E-52862) is a selective sigma-1 receptor (σ1R) antagonist with a reported binding affinity of Ki = 17.0 ± 7.0 nM for human σ1 receptor , selective over the sigma-2 receptor and against a panel of other 170 receptors, enzymes, transporters and ion channels.
Targets
σ1R [1]
()
17 nM(Ki)
In vitro

S1RA behaves as a highly selective σ1 receptor antagonist. It shows high affinity for human (Ki= 17 nM) and guinea pig (Ki= 23.5 nM) σ1 receptors but no significant affinity for the σ2 receptors (Ki > 1000 nM for guinea pig and rat σ2 receptors). It has moderate affinity (Ki= 328 nM) and antagonistic activity, with very low potency (IC50= 4700 nM) against human 5-HT2B receptor. S1RA shows no significant affinity (Ki > 1 µM or % inhibition at 1 µM < 50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes)[1].

In vivo

S1RA crosses the blood-brain barrier and binds to σ1 receptors in the CNS[1].

Protocol

Solubility (25°C)

In vitro DMSO 67 mg/mL (198.56 mM)
Water 67 mg/mL (198.56 mM)
Ethanol 19 mg/mL (56.3 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 337.42
Formula

C20H23N3O2

CAS No. 878141-96-9
Storage powder
in solvent
Synonyms E-52862
Smiles CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4

In vivo Formulation Calculator (Clear solution)

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Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

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Molecular Weight Calculator

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID