Monlunabant
Based on 1 publication(s) in Google Scholar
Monlunabant ((S)-MRI-1891) is an orally active antagonist for cannabinoid receptor 1 (CB1), binds to hCB1 and hCB2 with Ki of 0.3 nM and 613 nM.
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- Pureza: 99.99%
- No. CAS: 2712480-46-9
- Fòrmula: C26H22ClF3N6O3S
- Peso molecular:591.00
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) Monlunabant
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Actividad biológica
CB1[1]
Monlunabant inhibits CB1-induced β-arrestin-2 recruitment (IC50 = 21 pM), suppresses G protein activation (IC50 = 6 nM)[1].
Monlunabant (0.3-30 nM, 60 min) enhances insulin secretion in INS-1 (832/13) cell, human and mouse islet cells under the presence of glucose (10 mM)[2].
Monlunabant (3 nM, 48 h) inhibits cytokine-induced apoptosis in human islets[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human islets
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Concentration:3 nM
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Incubation Time:48 h
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Result:Inhibited apoptosis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57Bl/6J wildtype mouse models[1]
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Dosage:1-10 mg/kg
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Administration:po for 6-28 days
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Result:Reduced appetite and body weight, improved obesity-induced insulin resistance and glucose tolerance.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2712480-46-9
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Appearance Solid
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Peso molecular 591.00
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Fòrmula C26H22ClF3N6O3S
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Color White to off-white
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SMILES
O=S(N/C(N1N=C(C2=CC=C(C=C2)Cl)[C@@H](C3=CC=CC=C3)C1)=N/C(NC(C)=O)=N)(C4=CC=C(C=C4)C(F)(F)F)=O
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Synonyms
(S)-MRI-1891; INV-202
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Behav Pharmacol
2025 Apr 1;36(2-3):156-160. PMID: 39969070
Solvente y solubilidad
DMSO : 100 mg/mL (169.20 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. 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. 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 (4.23 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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.
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.
Pureza y Documentación
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Ficha de datos (277 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)
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- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Liu Z, et al., Functional Selectivity of a Biased Cannabinoid-1 Receptor (CB1R) Antagonist. ACS Pharmacol Transl Sci. 2021 Apr 8;4(3):1175-1187. [Content Brief]
[2]. Ghosh A, et al., A peripherally restricted cannabinoid-1 receptor inverse agonist promotes insulin secretion and protects from cytokine toxicity in human pancreatic islets. Eur J Pharmacol. 2023 Apr 5;944:175589 [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. 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 | 1.6920 mL | 8.4602 mL | 16.9205 mL | 42.3012 mL |
| 5 mM | 0.3384 mL | 1.6920 mL | 3.3841 mL | 8.4602 mL | |
| 10 mM | 0.1692 mL | 0.8460 mL | 1.6920 mL | 4.2301 mL | |
| 15 mM | 0.1128 mL | 0.5640 mL | 1.1280 mL | 2.8201 mL | |
| 20 mM | 0.0846 mL | 0.4230 mL | 0.8460 mL | 2.1151 mL | |
| 25 mM | 0.0677 mL | 0.3384 mL | 0.6768 mL | 1.6920 mL | |
| 30 mM | 0.0564 mL | 0.2820 mL | 0.5640 mL | 1.4100 mL | |
| 40 mM | 0.0423 mL | 0.2115 mL | 0.4230 mL | 1.0575 mL | |
| 50 mM | 0.0338 mL | 0.1692 mL | 0.3384 mL | 0.8460 mL | |
| 60 mM | 0.0282 mL | 0.1410 mL | 0.2820 mL | 0.7050 mL | |
| 80 mM | 0.0212 mL | 0.1058 mL | 0.2115 mL | 0.5288 mL | |
| 100 mM | 0.0169 mL | 0.0846 mL | 0.1692 mL | 0.4230 mL |
Monlunabant Related Classifications
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