S1RA
Based on 3 publication(s) in Google Scholar
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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- Purity : 99.67%
- CAS No.: 878141-96-9
- 화학식: C20H23N3O2
- 분자량:337.42
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Cutamesine dihydrochlorideσ1R Agonist -
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BD-1063 dihydrochlorideσ-1R Antagonist -
HY-18099A
S1RA hydrochlorideσ1R Antagonist -
HY-14221
SiramesineSigma-2 Receptor Agonist -
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4-IBPσ1 Receptor Agonist
Publications Citing Use of MedChemExpress (MCE) S1RA
MoreAll Sigma Receptor Isoforms
MoreAll 5-HT Receptor Isoforms
More
Biological Activity
제품 설명
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human σ1R 17 nM (Ki) |
5-HT2B Receptor |
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
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
>10 μM
Compound: 1
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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
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[PMID: 25658964] |
| HEK293 | IC50 |
>10 μM
Compound: 28, S1RA, E-52862
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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
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[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.
In Vivo
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.
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Animal Model:WT and TRPA1 KO mice with AITC (10 µl at 10 mM) in their hind paws[2]
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Dosage:40 mg/kg
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Administration:IP; single dose; 24-h before evaluation
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Result:Produced a substantial reduction in pain-related responses to intradermal AITC in WT mice.
Chemical Information
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CAS No. 878141-96-9
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Appearance Solid
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분자량 337.42
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화학식 C20H23N3O2
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Color Off-white to yellow
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SMILES
CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3
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Synonyms
E-52862
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Eur J Med Chem
Benzylaminofentanyl derivates: Discovery of bifunctional μ opioid and σ1 receptor ligands as novel analgesics with reduced adverse effects. [Abstract]2022 Nov 5:241:114649. PMID: 35961067 -
Biomolecules
Sigma-1 Receptor Modulates CFA-Induced Inflammatory Pain via Sodium Channels in Small DRG Neurons. [Abstract]2025 Jan 6;15(1):73. PMID: 39858467 -
Neuropharmacology
Novel mechanism of hypidone hydrochloride (YL-0919) in Parkinson's disease: inhibiting neuronal ferroptosis by targeting the Sigma1R-PI3K-AKT-ACSL4 axis. [Abstract]2026 Jul 1:292:110950. PMID: 41887568
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
순도&문서
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Data Sheet (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Díaz JL, et al. Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862). J Med Chem. 2012 Oct 11;55(19):8211-24. [Content Brief]
[2]. Aida Marcotti, et al. TRPA1 modulation by Sigma-1 receptor prevents oxaliplatin-induced painful peripheral neuropathy. Brain. 2023 Feb 13;146(2):475-491. [Content Brief]
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 |
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| 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 |
S1RA Related Classifications
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