PRE-084 hydrochloride
Based on 14 publication(s) in Google Scholar
PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.
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- Pureté : 99.92%
- CAS No.: 75136-54-8
- Formule: C19H28ClNO3
- Masse moléculaire:353.88
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Stockage:
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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PRE-084 hydrochloride
More- J Adv Res. 2026 Aug 1:S2090-1232(26)00605-3.
- Acta Pharmacol Sin. 2020 Apr;41(4):499-507. [Abstract]
- EMBO Mol Med. 2022 Jul 7;14(7):e15373. [Abstract]
- Inflamm Res. 2025 Sep 4;74(1):117. [Abstract]
- Cells. 2023 Jan 3;12(1):197. [Abstract]
- Int Immunopharmacol. 2025 Dec 10:167:115677. [Abstract]
- Biomolecules. 2025 Jan 6;15(1):73. [Abstract]
- Int Immunopharmacol. 2024 Feb 15:128:111524. [Abstract]
- Molecules. 2023 Jan 2;28(1):390. [Abstract]
- Exp Neurol. 2022 Jun:352:114034. [Abstract]
- Brain Res Bull. 2025 Feb:221:111226. [Abstract]
- Behav Brain Res. 2025 Apr 27:484:115493. [Abstract]
- Int J Gen Med. 2025 Apr 4:18:1917-1931. [Abstract]
- Aging (Albany NY). 2020 May 14;12(10):9041-9065. [Abstract]
Customer Validation & Images
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ELISA
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Cell Imaging/Staining
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WB
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IF
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In Vivo Efficacy Study
Voir tous les produits spécifiques à Isoform Sigma Receptor
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Activité biologique
Description
IC50 & Target
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eNOS |
Sigma 1 Receptor |
In Vitro
PRE-084 hydrochloride (0.1-100 μM; 24 h) protects cultured cortical neurons against β-amyloid toxicity (maximally neuroprotective at 10 μM) and reduces the levels of proapoptotic protein Bax at 10 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Cortical cells (βAP(25-35)-induced neurotoxicity model)
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Concentration:0.1-100 µM
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Incubation Time:24 h
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Result:Reduced neuronal toxicity in a bell shaped-manner and is maximally neuroprotective at 10 µM.
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Cell Line:Cortical cells (βAP(25-35)-induced neurotoxicity model)
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Concentration:10 µM
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Incubation Time:24 h
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Result:Reduced the levels of proapoptotic protein Bax in cortical neurons induced by βAP(25-35).
In Vivo
PRE-084 hydrochloride (1 mg/kg; i.p.; single) protects the heart by activating the Akt eNOS pathway in myocardial infarction model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wobbler mice (4-week-old)[2].
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Dosage:0.25 mg/kg
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Administration:Intraperitoneal injection; 3 times a week for 8 weeks.
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Result:Significantly improved ameliorated paw abnormality from week 4, and notably improved paw grip strength at week 5.
Reduced the number of reactive astrocytes whereas increased the number of pan-macrophage marker CD68-positive cells and CD206+ cells involved in tissue restoration.
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Animal Model:Adult male Sprague‑Dawley rats (220-250 g; myocardial infarction model)[3].
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Dosage:1 mg/kg
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Administration:Intraperitoneal injection; single.
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Result:Significantly decreased the degree of myocardial apoptosis.
Led to significantly increased expression of p‑Akt and p‑eNOS.
Chemical Information
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CAS No. 75136-54-8
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Appearance Solid
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Masse moléculaire 353.88
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Formule C19H28ClNO3
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Color White to off-white
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SMILES
O=C(C1(C2=CC=CC=C2)CCCCC1)OCCN3CCOCC3.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (14)
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Journal Impact Factor
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Most Recent
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Acta Pharmacol Sin
Development and characterization of an inducible Dicer conditional knockout mouse model of Parkinson's disease: validation of the antiparkinsonian effects of a sigma-1 receptor agonist and dihydromyricetin. [Abstract]2020 Apr;41(4):499-507. PMID: 32112040
PRE-084 hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Apr;41(4):499-507. [Abstract]
Chronic PRE-084 hydrochloride (1 mg/kg; once daily for 8 weeks) treatment alleviates DA neuron loss in Dicer cKO mice. TH and Iba1 immunostaining. Representative photomicrographs were shown at ×20 magnification (scale bars, 100 μm).
PRE-084 hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Apr;41(4):499-507. [Abstract]
Chronic DHM and PRE-084 hydrochloride treatment attenuated the development of PD-like motor functions in Dicer cKO mice. All mice were injected with 10 mg/mL tamoxifen (i.p.) twice a day for 5 days. Meanwhile, mice also received daily injections of 10 mg/kg of DHM, 1 mg/kg of PRE-084 hydrochloride, or vehicle, respectively, for 8 weeks. Behavioral tests were conducted every other week starting from week 6. The pole test and rotarod test were performed in mice at indicated times with or without DHM and PRE-084 hydrochloride injections, respectively.
PRE-084 hydrochloride purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Apr;41(4):499-507. [Abstract]
PRE-084 hydrochloride (1 mg/kg; once daily for 8 weeks) significantly restored TH expression in Dicer cKO mice.
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EMBO Mol Med
Sigma-1 receptor attenuates osteoclastogenesis by promoting ER-associated degradation of SERCA2. [Abstract]2022 Jul 7;14(7):e15373. PMID: 35611810
PRE-084 hydrochloride purchased from MedChemExpress. Usage Cited in: EMBO Mol Med. 2022 Jul 7;14(7):e15373. [Abstract]
TRAP staining detected osteoclastogenesis of BMMs treated with different Sigmar1 agonists (PRE-084 hydrochloride, et al., 10 μM; 5 days) or vector. The results showed all of these agonists could reduce the osteoclast number and size.
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Inflamm Res
Sigma-1 receptor activation by PRE-084 attenuates sepsis-associated encephalopathy by targeting microglial p38 MAPK-mediated neuroinflammation and neuronal endoplasmic reticulum stress. [Abstract]2025 Sep 4;74(1):117. PMID: 40903700
PRE-084 hydrochloride purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2025 Sep 4;74(1):117. [Abstract]
PRE-084 hydrochloride (10 mg/kg; i.v.; once daily for 3 days) reduced inflammatory cytokines in CLP-induced sepsis-associated encephalopathy in mice.
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Cells
Sigma-1 Receptor as a Protective Factor for Diabetes-Associated Cognitive Dysfunction via Regulating Astrocytic Endoplasmic Reticulum-Mitochondrion Contact and Endoplasmic Reticulum Stress. [Abstract]2023 Jan 3;12(1):197. PMID: 36611988 -
Int Immunopharmacol
Sigma-1 receptor activation ameliorates age-related postoperative cognitive dysfunction by attenuating endoplasmic reticulum stress and neuroinflammation. [Abstract]2025 Dec 10:167:115677. PMID: 41076930 -
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 -
Int Immunopharmacol
Hypidone hydrochloride (YL-0919) protects mice from meningitis via Sigma1R-STAT1-NLRP3-GSDMD pathway. [Abstract]2024 Feb 15:128:111524. PMID: 38232537 -
Molecules
Sigma-1 Receptor Activation Improves Oligodendrogenesis and Promotes White-Matter Integrity after Stroke in Mice with Diabetic Mellitus. [Abstract]2023 Jan 2;28(1):390. PMID: 36615583 -
Exp Neurol
MiR-153 downregulation alleviates PTSD-like behaviors and reduces cell apoptosis by upregulating the Sigma-1 receptor in the hippocampus of rats exposed to single-prolonged stress. [Abstract]2022 Jun:352:114034. PMID: 35259352
PRE-084 hydrochloride purchased from MedChemExpress. Usage Cited in: Exp Neurol. 2022 Jun:352:114034. [Abstract]
The therapeutic effect of the σ-1R agonist PRE-084 hydrochloride (0.6 mg/kg; i.p.) in SPS rats is blocked by the mTOR signaling pathway inhibitor Rapamycin.
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Brain Res Bull
Pharmacological modulation of Sigma-1 receptor ameliorates pathological neuroinflammation in rats with diabetic neuropathic pain via the AKT/GSK-3β/NF-κB pathway. [Abstract]2025 Feb:221:111226. PMID: 39870326 -
Behav Brain Res
Sigma-1 receptor agonist PRE-084 increases BDNF by activating the ERK/CREB pathway to rescue learning and memory impairment caused by type II diabetes. [Abstract]2025 Apr 27:484:115493. PMID: 39986614 -
Int J Gen Med
Sigma-1 Receptor Rescues Autophagy Through AMPK/mTOR Signaling Pathway in Sepsis-Induced Acute Kidney Injury. [Abstract]2025 Apr 4:18:1917-1931. PMID: 40201929 -
Aging (Albany NY)
Sigma-1 receptor is involved in diminished ovarian reserve possibly by influencing endoplasmic reticulum stress-mediated granulosa cells apoptosis. [Abstract]2020 May 14;12(10):9041-9065. PMID: 32409627
Solvant et solubilité
In Vitro:
H2O : 33.33 mg/mL (94.18 mM; ultrasonic and warming and heat to 60°C)
DMSO : 17.5 mg/mL (49.45 mM; Need ultrasonic; 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 (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.
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: ≥ 2.08 mg/mL (5.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
Protocole
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Marrazzo A, et al. Neuroprotective effects of sigma-1 receptor agonists against beta-amyloid-induced toxicity. Neuroreport. 2005 Aug 1;16(11):1223-6. [Content Brief]
[2]. Peviani M, et al. Neuroprotective effects of the Sigma-1 receptor (S1R) agonist PRE-084, in a mouse model of motor neuron disease not linked to SOD1 mutation. Neurobiol Dis. 2014 Feb;62:218-32. [Content Brief]
[3]. Gao QJ, et al. Sigma-1 Receptor Stimulation with PRE-084 Ameliorates Myocardial Ischemia-Reperfusion Injury in Rats. Chin Med J (Engl). 2018 Mar 5;131(5):539-543. [Content Brief]
[4]. Su TP, et al. Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand. J Pharmacol Exp Ther. 1991 Nov;259(2):543-50. [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 |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 2.8258 mL | 14.1291 mL | 28.2582 mL | 70.6454 mL |
| 5 mM | 0.5652 mL | 2.8258 mL | 5.6516 mL | 14.1291 mL | |
| 10 mM | 0.2826 mL | 1.4129 mL | 2.8258 mL | 7.0645 mL | |
| 15 mM | 0.1884 mL | 0.9419 mL | 1.8839 mL | 4.7097 mL | |
| 20 mM | 0.1413 mL | 0.7065 mL | 1.4129 mL | 3.5323 mL | |
| 25 mM | 0.1130 mL | 0.5652 mL | 1.1303 mL | 2.8258 mL | |
| 30 mM | 0.0942 mL | 0.4710 mL | 0.9419 mL | 2.3548 mL | |
| 40 mM | 0.0706 mL | 0.3532 mL | 0.7065 mL | 1.7661 mL | |
| H2O | 50 mM | 0.0565 mL | 0.2826 mL | 0.5652 mL | 1.4129 mL |
| 60 mM | 0.0471 mL | 0.2355 mL | 0.4710 mL | 1.1774 mL | |
| 80 mM | 0.0353 mL | 0.1766 mL | 0.3532 mL | 0.8831 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.
PRE-084 hydrochloride Related Classifications
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