Cat. No.: HY-18100A

PRE-084 hydrochloride

13 Cited Publications

Customer Review

Based on 13 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.

For research use only. We do not sell to patients.

Purity: 99.92%
CAS No.: 75136-54-8
Formula: C₁₉H₂₈ClNO₃
Molecular Weight:353.88

Storage:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

PRE-084 hydrochloride Chemical Structure

CAS No.: 75136-54-8

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (13)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

eNOS	Sigma 1 Receptor

All Sigma Receptor Isoforms :

All Akt Isoforms :

All NO Synthase Isoforms :

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.

Cell Viability Assay^[1]

Cell Line:

Cortical cells (βAP(25-35)-induced neurotoxicity model)
Concentration:

0.1-100 µM
Incubation Time:

24 h
Result:

Reduced neuronal toxicity in a bell shaped-manner and is maximally neuroprotective at 10 µM.

Western Blot Analysis^[1]

Cell Line:

Cortical cells (βAP(25-35)-induced neurotoxicity model)
Concentration:

10 µM
Incubation Time:

24 h
Result:

Reduced the levels of proapoptotic protein Bax in cortical neurons induced by βAP(25-35).

In Vivo

PRE-084 hydrochloride (0.25 mg/kg; i.p.; 3 times a week for 8 weeks) displays beneficial effects on motor performance (improves motor neuron survival, ameliorates paw abnormality and grip strength performance) in wobbler mice, and shows neuroprotective effects (increases the levels of BDNF in the gray matter)^[2].
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.

Animal Model:

Wobbler mice (4-week-old)^[2].
Dosage:

0.25 mg/kg
Administration:

Intraperitoneal injection; 3 times a week for 8 weeks.
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.

Animal Model:

Adult male Sprague‑Dawley rats (220-250 g; myocardial infarction model)^[3].
Dosage:

1 mg/kg
Administration:

Intraperitoneal injection; single.
Result:

Significantly decreased the degree of myocardial apoptosis.
Led to significantly increased expression of p‑Akt and p‑eNOS.

Chemical Information

CAS No. 75136-54-8
Appearance Solid
Molecular Weight 353.88
Formula C₁₉H₂₈ClNO₃
Color White to off-white
SMILES

O=C(C1(C2=CC=CC=C2)CCCCC1)OCCN3CCOCC3.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (13)

All ELISACell Imaging/StainingIFIn Vivo Efficacy StudyWB

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Journal Impact Factor

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.
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.
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.
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
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

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
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.
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
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

Solvent & Solubility

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8258 mL

14.1291 mL

28.2582 mL

5 mM

0.5652 mL

2.8258 mL

5.6516 mL

10 mM

0.2826 mL

1.4129 mL

2.8258 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 2.08 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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (5.88 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

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.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Keywords

PRE-084 hydrochloride

13 Cited Publications

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PRE-084 hydrochloride

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

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Publications Citing Use of MedChemExpress (MCE) PRE-084 hydrochloride

All Sigma Receptor Isoforms

All Akt Isoforms

All NO Synthase Isoforms

Biological Activity

Chemical Information

Publications (13)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

PRE-084 hydrochloride Related Classifications

Cat. No.: HY-18100A