PRE-084 hydrochloride |
Katalog-Nr.GC14960
One-Click Copy Product Info
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PRE-084-Hydrochlorid ist ein hochselektiver σ1-Rezeptor (S1R)-Agonist mit einem IC50-Wert von 44 nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 75136-54-8
Sample solution is provided at 25 µL, 10mM.
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PRE-084 hydrochloride is a highly selective sigma-1 receptor (S1R) agonist with an IC50 value of 44nM[1]. PRE-084 hydrochloride has demonstrated broad neuroprotective and anti-inflammatory effects across multiple models of neurodegeneration and neuroinflammation such as Parkinson’s disease and amyotrophic lateral sclerosis[3][4][5].
In vitro, PRE-084 hydrochloride (10µM) treatment on dorsal root ganglia (DRG) neurons isolated from CFA-treated rats for 30min led to a decrease in the fast sodium current, which was associated with a diminished action potential (AP) peak and maximum depolarizing rate (MDR), as well as an increased rheobase[2]. PRE-084 hydrochloride (0.1–20µM) and β-amyloid fragment 25–35 (25µM) were co-applied to rat cortical neuronal cultures for 24h. PRE-084 hydrochloride reduced neuronal toxicity in a bell shaped-manner with maximally neuroprotective effect at 10µM and blocked the β-amyloid-induced rise in the pro-apoptotic protein Bax[3]. PRE-084 hydrochloride (2.5μg/mL) applied on BV-2 cells when cells challenged with S. pneumoniae at 20 MOI for 6h exerted anti-inflammatory effect by reducing the expression of phosphorylated STAT1 (p-STAT1) and NLRP3[4].
In vivo, PRE-084 hydrochloride (0.25µg/g) was administered intraperitoneally into the wobbler (wr) mouse model of spontaneous motor-neuron degeneration three times per week from the 4th to the 12th week of age. PRE-084 hydrochloride treatment increased the number of surviving motor neurons, raised cervical spinal-cord BDNF levels, while attenuating reactive astrogliosis and shifting microglia/macrophages toward a CD68⁺ and CD206⁺ tissue-repair phenotype in wr mice[5]. PRE-084 hydrochloride (3mg/kg) administrated intraperitoneally into streptozotocin induced diabetic rats once a day for a week enhanced vasoconstrictor and platelet aggregator and reduced vasodilator and anti-aggregator cyclooxygenase product formation[6]. PRE-084 hydrochloride (1mg/kg) were administered into myocardial ischemia/reperfusion model rats 1h before operation. PRE-084 hydrochloride preserved cardiac function and reduced myocardial apoptosis through the activation of Akt and eNOS[7].
References:
[1] Su T P, Wu X Z, Cone E J, 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.
[2] Song Y L, Xu Z F, Zhang L P, et al. Sigma-1 Receptor Modulates CFA-Induced Inflammatory Pain via Sodium Channels in Small DRG Neurons. Biomolecules. 2025 Jan 6;15(1):73.
[3] Marrazzo A, Caraci F, Salinaro E T, et al. Neuroprotective effects of sigma-1 receptor agonists against beta-amyloid-induced toxicity. Neuroreport. 2005 Aug 1;16(11):1223-6.
[4] Gao Z F, Xie S, Wang L Y, et al. Hypidone hydrochloride (YL-0919) protects mice from meningitis via Sigma1R-STAT1-NLRP3-GSDMD pathway. Int Immunopharmaco. 2024 Feb 15:128:111524.
[5] Peviani M, Salvaneschi E, Bontempi L, 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.
[6] Váczi S, Barna L, Laczi K, et al. Effects of sub-chronic, in vivo administration of sigma-1 receptor ligands on platelet and aortic arachidonate cascade in streptozotocin-induced diabetic rats. PLoS One. 2022 Nov 17;17(11):e0265854.
[7] Gao Q J, Yang B, Chen J, 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.
| Cell experiment [1]: | |
Cell lines | Rat dorsal root ganglion (DRG) neurons |
Preparation Method | DRG neurons were collected from six sham rats and six rats after three days of CFA injection One portion was used as control, and the other was treated with PRE-084 hydrochloride (10µM) for 30min before further processing. |
Reaction Conditions | 10μM; 30min |
Applications | Activation of Sig-1R through PRE-084 hydrochloride led to a decrease in the fast sodium current in isolated DRG neurons from CFA-treated rats, which was associated with a diminished action potential (AP) peak and maximum depolarizing rate (MDR), as well as an increased rheobase. PRE-084 hydrochloride was also observed to enhance the slow component of the sodium current, resulting in hyperpolarization of the threshold potential and an increase in AP firing frequency. |
| Animal experiment [2]: | |
Animal models | Sprague-Dawley rat |
Preparation Method | The rats were injected intraperitoneally with PRE-084 hydrochloride or saline (1mg/kg). One hour later, ischemia was induced by ligation at the left anterior descending coronary artery. Rats were subjected to 30min of myocardial ischemia and 24h of reperfusion. |
Dosage form | 1mg/kg; i.p; 1h before myocardial ischemia operation |
Applications | PRE-084 hydrochloride preserved cardiac function and reduced myocardial apoptosis through the activation of Akt and eNOS. |
References: | |
| Cas No. | 75136-54-8 | SDF | |
| Chemical Name | 2-morpholinoethyl 1-phenylcyclohexanecarboxylate hydrochloride | ||
| Canonical SMILES | O=C(C1(C2=CC=CC=C2)CCCCC1)OCCN3CCOCC3.Cl | ||
| Formula | C19H27NO3.HCl | M.Wt | 353.89 |
| Löslichkeit | ≥ 17.3mg/mL in DMSO with gentle warming | Storage | Store at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8257 mL | 14.1287 mL | 28.2574 mL |
| 5 mM | 565.1 μL | 2.8257 mL | 5.6515 mL |
| 10 mM | 282.6 μL | 1.4129 mL | 2.8257 mL |
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Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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Average Rating: 5 (Based on Reviews and 8 reference(s) in Google Scholar.)