Cat. No.: HY-13101

MCOPPB trihydrochloride

Name: MCOPPB trihydrochloride
Brand: MedChemExpress
SKU: HY-13101
Price: 57.00 USD
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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.

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Pureté : 99.98%
CAS No.: 1108147-88-1
Formule: C₂₆H₄₃Cl₃N₄
Masse moléculaire:518.01

Stockage:

4°C, sealed storage, away from moisture

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

MCOPPB trihydrochloride Chemical Structure

CAS No.: 1108147-88-1

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Fluorescent Dye

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

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

IC₅₀ & Target

^[1]

NOP Receptor/ORL1

Voir tous les produits spécifiques à Isoform Opioid Receptor :

In Vitro

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.

Cell Viability Assay^[1]

Cell Line:

aphidicolin-induced senescent human MRC5 fibroblasts, non-senescent proliferating human MRC5 fibroblasts
Concentration:

10 μM
Incubation Time:

5 days
Result:

Showed preferential toxicity towards aphidicolin-induced senescent MRC5 fibroblasts compared to non-senescent proliferating MRC5 fibroblasts.

Cell Viability Assay^[1]

Cell Line:

doxorubicin-induced senescent human HepG2 hepatocellular carcinoma cells, doxorubicin-induced senescent human Huh-7 hepatocellular carcinoma cells
Concentration:

0.125-5 μM
Incubation Time:

24 h
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.

Western Blot Analysis^[3]

Cell Line:

H9C2 cells
Concentration:

0.5 µM (MCOPPB trihydrochloride); 100 nM (ET-1); 10 µM (ORL1 antagonist)
Incubation Time:

24 h (ET-1 added after MCOPPB trihydrochloride); 30 min (ORL1 antagonist added after ET-1); 3 days (total)
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.

In Vivo

MCOPPB trihydrochloride (2.5-5 mg/kg; i.p.; 5 consecutive days followed by 2 days rest; 21 days) exerts potent, tissue-specific senolytic effects in peripheral tissues (white adipose tissue and liver) of aging male C57BL/6 mice^[1].
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.

Animal Model:

C57BL/6 Mice with Age-related senescence model (male, 20 weeks old)^[1]
Dosage:

5 mg/kg (first week); 2.5 mg/kg (subsequent 2 weeks)
Administration:

i.p.; 5 consecutive days followed by 2 days rest; 21 days
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.

Related Protocols :

Chemical Information

CAS No. 1108147-88-1
Appearance Solid
Masse moléculaire 518.01
Formule C₂₆H₄₃Cl₃N₄
Color White to off-white
SMILES

CC1(N2CCC(N3C4=CC=CC=C4N=C3[C@H]5CNCCC5)CC2)CCCCCCC1.[H]Cl.[H]Cl.[H]Cl
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

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

Solvant et solubilité

In Vitro:

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)

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

1.9305 mL

9.6523 mL

19.3046 mL

5 mM

0.3861 mL

1.9305 mL

3.8609 mL

10 mM

0.1930 mL

0.9652 mL

1.9305 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.5 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.

Protocol 2

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.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (4.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (286 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)
Instruction de manipulation (2659 KB)

Références

[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]

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	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

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MCOPPB trihydrochloride

1 Cited Publications

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MCOPPB trihydrochloride

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Voir tous les produits spécifiques à Isoform Opioid Receptor