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> S1RA [878141-96-9]

S1RA [878141-96-9]

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Referência HY-18099-5mg

Tamanho : 5mg

Marca : MedChemExpress

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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.
Masse moléculaire

337.42

Formule

C20H23N3O2
CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
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.

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.
Pureté et documentation
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