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

S1RA hydrochloride  (Synonyms: E-52862 hydrochloride)

Cat. No.: HY-18099A Purity: 99.85%
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S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization.

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S1RA hydrochloride Chemical Structure

S1RA hydrochloride Chemical Structure

CAS No. : 1265917-14-3

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of S1RA hydrochloride:

S1RA hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE S1RA hydrochloride

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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

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Description

S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization[1][2].

IC50 & Target

Sigma 1 Receptor

 

In Vitro

S1RA hydrochloride (0.1-10000 nM) shows high affinity to human and guinea pig σ1Rs with Ki values of 17 and 23.5 nM, respectively[1].
S1RA hydrochloride (0.1-10000 nM) shows affinity to human σ2R with Ki values of 9.3 μM[1].
S1RA hydrochloride shows affinity to human 5-HT2B receptor with a Ki value of 328 nM and an IC50 value of 4.7 μM[1].

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

S1RA hydrochloride Related Antibodies
In Vivo

S1RA hydrochloride (i.p. 16-80 mg/kg or oral administration 32-128 mg/kg; once) dose-dependently inhibits formalin-induced nociception, capsaicin-induced mechanical hypersensitivity and sciatic nerve injury-induced mechanical and thermal hypersensitivity of mice[1].

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

Animal Model: Male CD1 mice[1]
Dosage: 32, 64, 128 and 160 mg/kg
Administration: Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once
Result: Reduced the permanence time on the rotating rod in rotarod test.
Animal Model: Male CD1 mice with formalin-evoked nociception[1]
Dosage: 20, 40 and 80 mg/kg
Administration: Intraperitoneal injection; 20, 40 and 80 mg/kg, once
Result: Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice.
Animal Model: Male CD1 mice with capsaicin-induced mechanical hypersensitivity[1]
Dosage: 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration)
Administration: Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once
Result: Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.
Molecular Weight

373.88

Formula

C20H24ClN3O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (267.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 16.67 mg/mL (44.59 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6747 mL 13.3733 mL 26.7465 mL
5 mM 0.5349 mL 2.6747 mL 5.3493 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • 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 (6.69 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 (6.69 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 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 110 mg/mL (294.21 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation
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 (sealed storage, away from moisture). 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
H2O / DMSO 1 mM 2.6747 mL 13.3733 mL 26.7465 mL 66.8664 mL
5 mM 0.5349 mL 2.6747 mL 5.3493 mL 13.3733 mL
10 mM 0.2675 mL 1.3373 mL 2.6747 mL 6.6866 mL
15 mM 0.1783 mL 0.8916 mL 1.7831 mL 4.4578 mL
20 mM 0.1337 mL 0.6687 mL 1.3373 mL 3.3433 mL
25 mM 0.1070 mL 0.5349 mL 1.0699 mL 2.6747 mL
30 mM 0.0892 mL 0.4458 mL 0.8916 mL 2.2289 mL
40 mM 0.0669 mL 0.3343 mL 0.6687 mL 1.6717 mL
DMSO 50 mM 0.0535 mL 0.2675 mL 0.5349 mL 1.3373 mL
60 mM 0.0446 mL 0.2229 mL 0.4458 mL 1.1144 mL
80 mM 0.0334 mL 0.1672 mL 0.3343 mL 0.8358 mL
100 mM 0.0267 mL 0.1337 mL 0.2675 mL 0.6687 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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S1RA hydrochloride 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:

S1RA1265917-14-3E-52862E52862E 52862Sigma Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine Receptorneuropathic painspinal sensitizationguinea pigformalincapsaicinCD1 miceInhibitorinhibitorinhibit

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