1. GPCR/G Protein Neuronal Signaling
  2. Cannabinoid Receptor Arrestin
  3. Monlunabant

Monlunabant  (Synonyms: (S)-MRI-1891; INV-202)

Cat. No.: HY-153800 Purity: 99.89%
Data Sheet Handling Instructions Technical Support

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.

For research use only. We do not sell to patients.

Monlunabant Chemical Structure

Monlunabant Chemical Structure

CAS No. : 2712480-46-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO In-stock
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25 mg In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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[1].

IC50 & Target

CB1[1]

In Vitro

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.

Apoptosis Analysis[2]

Cell Line: human islets
Concentration: 3 nM
Incubation Time: 48 h
Result: Inhibited apoptosis.
In Vivo

Monlunabant (1-10 mg/kg, po for 6-28 days) improves obesity-related insulin resistance in C57Bl/6J wildtype mouse models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57Bl/6J wildtype mouse models[1]
Dosage: 1-10 mg/kg
Administration: po for 6-28 days
Result: Reduced appetite and body weight, improved obesity-induced insulin resistance and glucose tolerance.
Molecular Weight

591.00

Formula

C26H22ClF3N6O3S

CAS No.
Appearance

Solid

Color

White to off-white

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6920 mL 8.4602 mL 16.9205 mL
5 mM 0.3384 mL 1.6920 mL 3.3841 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation
References

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
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Monlunabant
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HY-153800
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