S1RA hydrochloride
Based on 3 publication(s) in Google Scholar
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.76%
- CAS 番号: 1265917-14-3
- 分子式: C20H24ClN3O2
- 分子量:373.88
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保管条件:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 S1RA hydrochloride
MoreSigma Receptor アイソフォーム固有の製品をすべて表示
More5-HT Receptor アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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Sigma 1 Receptor |
5-HT2B Receptor |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male CD1 mice[1]
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Dosage:32, 64, 128 and 160 mg/kg
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Administration:Intraperitoneal injection; 32, 64, 128 and 160 mg/kg, once
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Result:Reduced the permanence time on the rotating rod in rotarod test.
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Animal Model:Male CD1 mice with formalin-evoked nociception[1]
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Dosage:20, 40 and 80 mg/kg
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Administration:Intraperitoneal injection; 20, 40 and 80 mg/kg, once
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Result:Dose-dependently showed analgesic effect on of formalin-evoked nociceptive behaviours of mice.
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Animal Model:Male CD1 mice with capsaicin-induced mechanical hypersensitivity[1]
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Dosage:16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration)
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Administration:Intraperitoneal injection or oral administration; 16, 32 and 64 mg/kg (i.p.); 32, 64 and 128 mg/kg (oral administration), once
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Result:Dose-dependently reversed capsaicin-induced mechanical hypersensitivity in mice.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1265917-14-3
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性状 Solid
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分子量 373.88
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分子式 C20H24ClN3O2
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Color White to off-white
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SMILES
CC1=CC(OCCN2CCOCC2)=NN1C3=CC(C=CC=C4)=C4C=C3.[H]Cl
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別名
E-52862 hydrochloride
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
溶剤 & 溶解度
体外:
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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 (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.
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.
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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
純度とドキュメンテーション
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データシート (279 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Romero L, et al. Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization. Br J Pharmacol. 2012 Aug;166(8):2289-306. [Content Brief]
[2]. Vidal-Torres A, et al. Effects of the selective sigma-1 receptor antagonist S1RA on formalin-induced pain behavior and neurotransmitter release in the spinal cord in rats. J Neurochem. 2014 Jan 3. [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 (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.
S1RA hydrochloride 関連分類
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