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S1RA Sigma Receptor antagonist

Name: S1RA
Brand: Selleck Chemicals
SKU: S6754
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S6754

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.

Chemical Structure

Molecular Weight: 337.42

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
HPLC
SDS
Datasheet

99.45

Related Targets	CXCR Hedgehog/Smoothened PKA Adrenergic Receptor AChR 5-HT Receptor Histamine Receptor Dopamine Receptor Ras KRas
Other Sigma Receptor Inhibitors	BD-1047 dihydrobromide Anavex 2-73 HCl Carbetapentane 4-IBP WQ 1 Siramesine Cutamesine Dihydrochloride BD1063 2HCL PRE-084 hydrochloride Ditolylguanidine

Solubility

In vitro
Batch:

DMSO : 67 mg/mL (198.56 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 67 mg/mL

Ethanol : 19 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	3.35mg/ml (9.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 67 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.48mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

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.

Chemical Information, Storage & Stability

Molecular Weight	337.42	Formula	C₂₀H₂₃N₃O₂	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	878141-96-9	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	E-52862			Smiles	CC1=CC(=NN1C2=CC3=CC=CC=C3C=C2)OCCN4CCOCC4

Mechanism of Action

Targets/IC₅₀/Ki	σ1R 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). This compound has moderate affinity (Ki= 328 nM) and antagonistic activity, with very low potency (IC50= 4700 nM) against human 5-HT2B receptor. It shows no significant affinity (Ki > 1 µM or % inhibition at 1 µM < 50%) for other additional 170 targets (receptors, transporters, ion channels and enzymes).
In vivo	This compound crosses the blood-brain barrier and binds to σ1 receptors in the CNS.
References	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3448894/

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