MCOPPB trihydrochloride
Based on 1 publication(s) in Google Scholar
MCOPPB trihydrochloride is a NOP/ORL1 G protein-coupled receptor agonist and autophagy inhibitor that can cross the blood-brain barrier. MCOPPB trihydrochloride clears senescent cells, regulates locomotion, lipid storage and immune responses, and inhibits fibrosis and angiogenesis. MCOPPB trihydrochloride blocks autophagic flux, induces changes in locomotion and lipid storage, and activates the stress-responsive immune transcription network, thereby improving post-infarction cardiac function and exerting anxiolytic effects. MCOPPB trihydrochloride can be applied to research fields such as aging-related diseases and ischemic heart failure.
For research use only. We do not sell to patients.
- Purity: 99.98%
- CAS No.: 1108147-88-1
- Formula: C26H43Cl3N4
- Molecular Weight:518.01
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MCOPPB trihydrochloride
MoreAll Opioid Receptor Isoforms
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Biological Activity
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NOP Receptor/ORL1 |
MCOPPB trihydrochloride (10 μM; 5 days) preferentially reduces viability of Aphidicolin (HY-N6733)-induced senescent human MRC5 fibroblasts while having less effect on non-senescent proliferating human MRC5 fibroblasts[1].
MCOPPB trihydrochloride (0.125-5 μM; 24 h) reduces viability of doxorubicin-induced senescent human HepG2 and Huh-7 hepatocellular carcinoma cells in a dose-dependent manner, with significant effects observed at concentrations ≥0.75 μM[1].
MCOPPB trihydrochloride (0.5 µM; 3 days total) downregulates NPPA and NPPB gene expression in ET-1-stimulated neonatal rat cardiomyocytes, an effect that is mediated via the ORL1 receptor[3].
MCOPPB trihydrochloride (0.5 µM; 3 days total) reduces ET-1-induced nuclear NFATc4 accumulation in H9C2 cells, an effect that is mediated via the ORL1 receptor[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:aphidicolin-induced senescent human MRC5 fibroblasts, non-senescent proliferating human MRC5 fibroblasts
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Concentration:10 μM
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Incubation Time:5 days
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Result:Showed preferential toxicity towards aphidicolin-induced senescent MRC5 fibroblasts compared to non-senescent proliferating MRC5 fibroblasts.
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Cell Line:doxorubicin-induced senescent human HepG2 hepatocellular carcinoma cells, doxorubicin-induced senescent human Huh-7 hepatocellular carcinoma cells
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Concentration:0.125-5 μM
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Incubation Time:24 h
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Result:Reduced viability of doxorubicin-induced senescent HepG2 and Huh-7 cells in a dose-dependent manner.
Identified 0.5 μM as the maximal cytostatic dose without cytotoxic effects.
Significantly reduced viability in Huh-7 cells at concentrations ≥0.75 μM compared to controls.
Significantly reduced viability in HepG2 cells at concentrations ≥0.75 μM compared to controls.
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Cell Line:H9C2 cells
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Concentration:0.5 µM (MCOPPB trihydrochloride); 100 nM (ET-1); 10 µM (ORL1 antagonist)
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Incubation Time:24 h (ET-1 added after MCOPPB trihydrochloride); 30 min (ORL1 antagonist added after ET-1); 3 days (total)
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Result:Decreased the ET-1-induced increase in nuclear NFATc4 protein expression in H9C2 cells.
Reversed the reduction of nuclear NFATc4 protein expression when co-treated with an ORL1 antagonist, significantly increasing nuclear NFATc4 expression.
MCOPPB trihydrochloride (2.5 mg/kg/day; i.p.; 5 days per week; 3 months) significantly improves cardiac function, reduces fibrosis, increases cardiomyocyte diameter, and induces angiogenesis in rats with post-myocardial infarction heart failure, with an ejection fraction of 67% at euthanasia[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 Mice with Age-related senescence model (male, 20 weeks old)[1]
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Dosage:5 mg/kg (first week); 2.5 mg/kg (subsequent 2 weeks)
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Administration:i.p.; 5 consecutive days followed by 2 days rest; 21 days
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Result:Reduced total ambulatory distance and border zone distance in the open-field test, and reduced mobility time in the forced swim test.
Reduced senescent cell burden by ~70% in visceral white adipose tissue and ~70% in hepatic parenchyma.
Induced a ~20% increase in adipocyte size in white adipose tissue, and mild hepatic steatosis with a steatosis score of 0.6.
Decreased the number of F4/80-positive hepatic macrophages by ~40% and double-positive F4/80+ β-gal+ senescent macrophages by ~60%.
Altered liver gene expression profiles, with enrichment in pathways related to immune response to pathogens, TREM1 signaling, mTOR signaling, hepatic stellate activation, and senescence, with TLR4 identified as a key nodal hub.
Chemical Information
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CAS No. 1108147-88-1
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Appearance Solid
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Molecular Weight 518.01
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Formula C26H43Cl3N4
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Color White to off-white
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SMILES
CC1(N2CCC(N3C4=CC=CC=C4N=C3[C@H]5CNCCC5)CC2)CCCCCCC1.[H]Cl.[H]Cl.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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RSC Med Chem
Probing non-peptide agonists binding at the human nociceptin/orphanin FQ receptor: a molecular modelling study. [Abstract]2024 Dec 10. PMID: 39790123
Solvent & Solubility
DMSO : 100 mg/mL (193.05 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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (4.83 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (286 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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Handling Instructions (2659 KB)
References
[1]. Raffaele M, et al. Nociceptin/orphanin FQ opioid receptor (NOP) selective ligand MCOPPB links anxiolytic and senolytic effects. Geroscience. 2022;44(1):463-483. [Content Brief]
[2]. Lacey M, et al. Autophagy revealed as a targetable vulnerability in senescent cells by cell painting phenotypic profiling: a mechanistic study of MCOPPB and related compounds. Geroscience. Published online April 30, 2026. [Content Brief]
[3]. Pathan SS, et al. Activation of a GPCR, ORL1 Receptor: A Novel Therapy to Prevent Heart Failure Progression. J Cardiovasc Dev Dis. 2024;11(11):355. Published 2024 Nov 5. [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 | 1 mM | 1.9305 mL | 9.6523 mL | 19.3046 mL | 48.2616 mL |
| 5 mM | 0.3861 mL | 1.9305 mL | 3.8609 mL | 9.6523 mL | |
| 10 mM | 0.1930 mL | 0.9652 mL | 1.9305 mL | 4.8262 mL | |
| 15 mM | 0.1287 mL | 0.6435 mL | 1.2870 mL | 3.2174 mL | |
| 20 mM | 0.0965 mL | 0.4826 mL | 0.9652 mL | 2.4131 mL | |
| 25 mM | 0.0772 mL | 0.3861 mL | 0.7722 mL | 1.9305 mL | |
| 30 mM | 0.0643 mL | 0.3217 mL | 0.6435 mL | 1.6087 mL | |
| 40 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2065 mL | |
| 50 mM | 0.0386 mL | 0.1930 mL | 0.3861 mL | 0.9652 mL | |
| 60 mM | 0.0322 mL | 0.1609 mL | 0.3217 mL | 0.8044 mL | |
| 80 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL | |
| 100 mM | 0.0193 mL | 0.0965 mL | 0.1930 mL | 0.4826 mL |
MCOPPB trihydrochloride Related Classifications
HY-13101 Related Classifications
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- MCOPPB trihydrochloride
- 1108147-88-1
- Opioid Receptor
- Autophagy
- Serine 346
- human Huh-7 hepatocellular carcinoma cells
- neonatal rat cardiomyocytes
- neonatal mouse cardiomyocytes
- blood-brain barrier
- NOP receptor
- human MRC5 fibroblasts
- human HepG2 hepatocellular carcinoma cells
- H9C2 cells
- NOP/ORL1 G protein-coupled receptor
- Inhibitor
- inhibitor
- inhibit