Home GPCR & G Protein Sigma Receptor antagonist S1RA For research use only.

S1RA

Synonyms: E-52862

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.

S1RA Chemical Structure

S1RA Chemical Structure

CAS: 878141-96-9

Selleck's S1RA has been cited by 1 publication

Purity & Quality Control

Batch: S675401 DMSO] 67 mg/mL] false] Water] 67 mg/mL] false] Ethanol] 19 mg/mL] false Purity: 99.45%
99.45

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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
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
In vivo

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

Chemical Information & Solubility

Molecular Weight 337.42 Formula

C20H23N3O2
CAS No. 878141-96-9 SDF --
Smiles CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 67 mg/mL ( (198.56 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 67 mg/mL

Ethanol : 19 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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