PRE-084
Based on 13 publication(s) in Google Scholar
PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.
For research use only. We do not sell to patients.
- CAS No.: 138847-85-5
- Formula: C19H27NO3
- Molecular Weight:317.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) PRE-084
More- 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 Oct 11:167:115677. [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 Jan 25:111226. [Abstract]
- Behav Brain Res. 2025 Apr 27:484:115493. [Abstract]
- Int J Gen Med. 2025 Apr 4:18:1917-1931. [Abstract]
- Aging. 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
All Sigma Receptor Isoforms
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Biological Activity
PRE-084 (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.
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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).
PRE-084 (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.
Showed 26.5% increase in the mean number of large-size NISSL-positive motor neurons.
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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. 138847-85-5
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Molecular Weight 317.42
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Formula C19H27NO3
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SMILES
O=C(OCCN1CCOCC1)C2(CCCCC2)C3=CC=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (13)
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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 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 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 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 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 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 Oct 11:167:115677. 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 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 Jan 25:111226. 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
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
Purity & Documentation
References
[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]
Calculators
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