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| 5mg |
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| Targets |
PRE-084 hydrochloride targets the sigma-1 receptor (S1R), a chaperone protein located at the endoplasmic reticulum-mitochondria interface that modulates various cellular processes including calcium signaling, oxidative stress, and neuroprotection. It has an IC50 of 44 nM in the sigma receptor assay and shows no significant affinity for PCP receptors (IC50 > 100,000 nM) or a variety of other receptor systems (IC50 > 10,000 nM).
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| ln Vitro |
PRE-084 hydrochloride (0.1-100 μM; 24 hours) protects cultured cortical neurons from beta-amyloid poisoning (maximal neuroprotection at 10 μM) and lowers pro-apoptotic proteins at 10 μM Bax level[1].
In vitro, PRE-084 hydrochloride is a highly selective agonist of the sigma-1 receptor with an IC50 of 44 nM. It exhibits good neuroprotective effects. It enhances BDNF-mediated trophic support. Its selectivity for sigma-1 receptors over other receptor systems is very high, with IC50 values greater than 10,000 nM for a variety of other receptor systems. |
| ln Vivo |
In wobbler mice, PRE-084 hydrochloride (0.25 mg/kg; i.p.; three times per week for eight weeks) demonstrated positive effects on locomotor performance (better grip performance, reduced paw abnormalities, and increased motor neuron survival), as well as neuroprotective effects (higher levels of BDNF in gray matter) [2]. ?By stimulating the Akt, PRE-084 hydrochloride (1 mg/kg; intraperitoneal injection; single dose) guards the heart.A model of myocardial infarction using the eNOS pathway [3].
In vivo, PRE-084 hydrochloride improves motor function and motor neuron survival in mice. It ameliorates myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway. It exhibits neuroprotective, antidepressant, and analgesic effects. These activities make it a valuable tool for studying sigma-1 receptor function in various disease models. |
| Enzyme Assay |
In vitro receptor binding assays for PRE-084 hydrochloride are conducted using radioligand binding with [³H]-haloperidol or [³H]-pentazocine in membrane preparations from tissues or cells expressing sigma-1 receptors. The compound is incubated with receptor membranes and radiolabeled ligand at varying concentrations, and IC50 or Ki values are calculated from competition curves.
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: Cortical cells (βAP(25-35) induced neurotoxicity model) Tested Concentrations: 0.1-100 µM Incubation Duration: 24 hrs (hours) Experimental Results: diminished neuronal toxicity in a bell-shaped manner and at 10 µM . Western Blot Analysis[1] Cell Types: Cortical cells (βAP(25-35)-induced neurotoxicity model) Tested Concentrations: 10 µM Incubation Duration: 24 h Experimental Results: βAP(25--induced pro-apoptotic protein Bax in cortical neurons Level diminished by 35). Cellular assays for PRE-084 hydrochloride are performed using neuronal cell lines or primary neurons. Cells are treated with compound concentrations ranging from 0.1 nM to 100 µM. Sigma-1 receptor activation is assessed by measuring downstream signaling events such as ERK phosphorylation, calcium mobilization, or mitochondrial function. Neuroprotection is assessed by measuring cell survival after exposure to toxic insults. |
| Animal Protocol |
Animal/Disease Models: Wobbler mouse (4 weeks old) [2].
Doses: 0.25 mg/kg Route of Administration: intraperitoneal (ip) injection; 3 times a week for 8 weeks. Experimental Results: Paw abnormalities were Dramatically improved from week 4 onwards, and paw grip strength was Dramatically improved by week 5. The number of reactive astrocytes diminished, while the number of panmacrophage markers CD68-positive cells and CD206+ cells involved in tissue repair increased. Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rat (220-250 g; myocardial infarction model) [3]. Doses: 1 mg/kg Route of Administration: intraperitoneal (ip) injection; single. Experimental Results: The degree of cardiomyocyte apoptosis was Dramatically diminished. Resulting in a significant increase in p-Akt and p-eNOS expression. In vivo animal studies for PRE-084 hydrochloride are conducted in rodent models of neurodegeneration, spinal cord injury, myocardial ischemia-reperfusion, pain, and depression. The compound is administered orally, intraperitoneally, or intrathecally. Endpoints include motor function tests, motor neuron survival, infarct size, pain threshold, and behavioral assessments. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of PRE-084 hydrochloride are not well characterized. The compound has a molecular weight of 353.88 and a molecular formula of C₁₉H₂₈ClNO₃. It is a crystalline solid. Standard PK studies in rodents would be required to determine half-life, bioavailability, and tissue distribution.
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| Toxicity/Toxicokinetics |
Toxicological data for PRE-084 hydrochloride are limited. As a research compound, it is designated for laboratory use only. No significant acute toxicity has been reported. Standard toxicity screening would involve acute and repeated-dose studies in rodents.
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| References |
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| Additional Infomation |
PRE-084 hydrochloride is a highly selective sigma-1 receptor agonist (IC50 = 44 nM). It exhibits neuroprotective effects and improves motor function and motor neuron survival in mice. It ameliorates myocardial ischemia-reperfusion injury in rats. It has a molecular weight of 353.88 and formula C₁₉H₂₈ClNO₃. It is not clinically approved.
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| Molecular Formula |
C19H27NO3.HCL
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| Molecular Weight |
353.884
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| Exact Mass |
353.175
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| CAS # |
75136-54-8
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| Related CAS # |
PRE-084;138847-85-5
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| PubChem CID |
11314197
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| Appearance |
White to off-white solid powder
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| LogP |
3.503
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
24
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| Complexity |
367
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
QUJWFJNHTBKCLU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H27NO3.ClH/c21-18(23-16-13-20-11-14-22-15-12-20)19(9-5-2-6-10-19)17-7-3-1-4-8-17;/h1,3-4,7-8H,2,5-6,9-16H2;1H
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| Chemical Name |
2-morpholin-4-ylethyl 1-phenylcyclohexane-1-carboxylate;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 34 mg/mL (~96.08 mM)
H2O : ~33.33 mg/mL (~94.18 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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