2. Neuronal Signaling GPCR/G Protein
  3. Sigma Receptor 5-HT Receptor
  4. S1RA

S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice.

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S1RA Chemical Structure

S1RA Chemical Structure

CAS No. : 878141-96-9

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 99 In-stock
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10 mM * 1 mL in DMSO USD 99 In-stock
Solid
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10 mg USD 165 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of S1RA:

S1RA Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE S1RA

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Sigma 1 Receptor Sigma 2 Receptor

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice[1][2].

IC50 & Target[1][3]

human σ1R

17 nM (Ki)

guinea pig σ1R

23.5 nM (Ki)

guinea pig σ2R

>1000 nM (Ki)

rat σ2R

9300 nM (Ki)

human 5-HT2B Receptor

328 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
CHO IC50
> 10 μM
Compound: 1
Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by whole cell patch clamp assay
Inhibition of human ERG expressed in CHO cells at -80 mV holding potential by whole cell patch clamp assay
[PMID: 25658964]
HEK293 IC50
> 10 μM
Compound: 28, S1RA, E-52862
Inhibition of human ERG transfected in HEK293 cell membranes by whole cell patch clamp assay
Inhibition of human ERG transfected in HEK293 cell membranes by whole cell patch clamp assay
[PMID: 22784008]
In Vitro

S1RA (E-52862; 100 µM; 4 h) inhibit intracellular calcium responses in TRPA1 expressing HEK293 cells[2].
S1RA (100 µM; 4 h) impairs the formation of TRPA1–Sigma-1R complexes and reduces TRPA1 expression at the plasma membrane[2].

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

S1RA Related Antibodies
In Vivo

S1RA (E-52862; 40 mg/kg; IP; single dose) produces a substantial reduction in pain-related responses to intradermal Allylisothiocyanate (AITC) in WT mice[2].
S1RA (40 mg/kg; IP; once a day for 11 consecutive days; starting 3 days before Oxaliplatin injection) prevents mechanical and cold hypersensitivity in Oxaliplatin (6 mg/kg; i.p.; Day 0, Day 2, Day 4)-treated mice[2].

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

Animal Model: WT and TRPA1 KO mice with AITC (10 µl at 10 mM) in their hind paws[2]
Dosage: 40 mg/kg
Administration: IP; single dose; 24-h before evaluation
Result: Produced a substantial reduction in pain-related responses to intradermal AITC in WT mice.
Molecular Weight

337.42

Formula

C20H23N3O2
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

1M HCl : 50 mg/mL (148.18 mM; ultrasonic and adjust pH to 1 with HCl)

DMSO : 33.33 mg/mL (98.78 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9637 mL 14.8183 mL 29.6367 mL
5 mM 0.5927 mL 2.9637 mL 5.9273 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.41 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.43%

SDS (251 KB)

COA (252 KB) HNMR (378 KB) LCMS (129 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / 1M HCl 1 mM 2.9637 mL 14.8183 mL 29.6367 mL 74.0916 mL
5 mM 0.5927 mL 2.9637 mL 5.9273 mL 14.8183 mL
10 mM 0.2964 mL 1.4818 mL 2.9637 mL 7.4092 mL
15 mM 0.1976 mL 0.9879 mL 1.9758 mL 4.9394 mL
20 mM 0.1482 mL 0.7409 mL 1.4818 mL 3.7046 mL
25 mM 0.1185 mL 0.5927 mL 1.1855 mL 2.9637 mL
30 mM 0.0988 mL 0.4939 mL 0.9879 mL 2.4697 mL
40 mM 0.0741 mL 0.3705 mL 0.7409 mL 1.8523 mL
50 mM 0.0593 mL 0.2964 mL 0.5927 mL 1.4818 mL
60 mM 0.0494 mL 0.2470 mL 0.4939 mL 1.2349 mL
80 mM 0.0370 mL 0.1852 mL 0.3705 mL 0.9261 mL
1M HCl 100 mM 0.0296 mL 0.1482 mL 0.2964 mL 0.7409 mL
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S1RA Related Classifications

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:

S1RA878141-96-9E-52862E52862E 52862Sigma Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorσ1 receptorσ1Rσ2Rantinociceptiveneuropathic painperipheral neuropathycolorectal cancer researchInhibitorinhibitorinhibit

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