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  3. Rimonabant Hydrochloride

Rimonabant Hydrochloride  (Synonyms: SR 141716A Hydrochloride)

Cat. No.: HY-14137 Purity: 99.31%
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Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

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

CAS No. : 158681-13-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg In-stock
100 mg In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Rimonabant Hydrochloride:

Top Publications Citing Use of Products

    Rimonabant Hydrochloride purchased from MedChemExpress. Usage Cited in: Cell. 2025 Dec 24;188(26):7547-7570.e45  [Abstract]

    FO of WT and CNR1 KO mice treated with Rimonabant (3 mg/kg; i.p.; single dose).

    Rimonabant Hydrochloride purchased from MedChemExpress. Usage Cited in: J Psychopharmacol. 2025 Jul 31:2698811251355603.  [Abstract]

    AUClog of low- and high-impulsive subpopulations for each treatment condition (Vehicle pre-treatment, Vehicle post-treatment, and Rimonabant (1 mg/kg; once every other day for 3 consecutive doses)). The results showed that Rimonabant reversed WIN55212-2-induced elevation in AUClog in rats via antagonism of the CB1 receptor.

    Rimonabant Hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2024 May 3;25(9):5012.  [Abstract]

    Fluorescent signal of Rimonabant at inhibiting GRABeCB2.0 basal fluorescence as determined by averaging ΔF/F0 between 4 and 5 min. The results showed that Rimonabant suppressed the fluorescent signal to below baseline levels in stable HEK293 cells expressing the GRABeCB2.0 sensor, indicating inverse agonist activity (EC50= 42 nM).

    Rimonabant Hydrochloride purchased from MedChemExpress. Usage Cited in: Autophagy. 2021 Nov;17(11):3592-3606.  [Abstract]

    Effect of various ion channel inhibitors on CBD-induced glioma cell death. U251 or LN18 cells were pretreated with Rimonabant (1 μM), SR144528 (1 μM), SEA0400 (10 μM), DIDS (10 μM), CID16020046 (1 μM), SKF96365 (1 μM), RuR (1 μM), mibefradil (2.5 uM), capsazepine (1 μM), or GSK2193874 (5 μM) for 1 h and then treated with CBD (30 μM) for 48 h. Cell viability was determined by the MTT assay. The results showed that Rimonabant failed to reverse the cell growth inhibitory effects induced by CBD.

    Rimonabant Hydrochloride purchased from MedChemExpress. Usage Cited in: Cell. 2019 Jan 24;176(3):636-648.e13.  [Abstract]

    Rimonabant was found to bind to MmpL3 with a dissociation constant (Kd value) of 29 μM.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an Ki of 1.8 nM. Rimonabant Hydrochloride (SR 141716A Hydrochloride) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

    IC50 & Target[1]

    CB1

    1.8 nM (Ki)

    Cellular Effect
    Cell Line Type Value Description References
    CHO IC50
    0.013 μM
    Compound: SR141716A
    Antagonist activity at CB1 receptor (unknown origin) expressed in CHO cells up to 10 uM incubated for 10 mins prior to CP55940 addition by calcium mobilization assay
    Antagonist activity at CB1 receptor (unknown origin) expressed in CHO cells up to 10 uM incubated for 10 mins prior to CP55940 addition by calcium mobilization assay
    [PMID: 25644673]
    CHO IC50
    9.8 μM
    Compound: SR141716A
    Antagonist activity at CB2 receptor (unknown origin) expressed in CHO cells up to 10 uM incubated for 10 mins prior to CP55940 addition by calcium mobilization assay
    Antagonist activity at CB2 receptor (unknown origin) expressed in CHO cells up to 10 uM incubated for 10 mins prior to CP55940 addition by calcium mobilization assay
    [PMID: 25644673]
    In Vitro

    Rimonabant could inhibit the growth of Mtb with an MIC of 54 μM. MmpL3, an anti-TB target, is the direct target of rimonabant[2].
    Rimonabant itself (10-12-10-3 M, 12 concentrations) inhibits the basal binding of [35S]GTPgS to human cortical membranes in a concentration dependent manner, with a -log IC50 of 4.7±0.2 (IC50 = 20 μM) and a maximal inhibition of 48±2%[3].

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

    In Vivo

    Rimonabant (10 mg/kg by gavage) is fed for 2 weeks to 3-month-old male obese Zucker rats as an impaired glucose tolerance model and for 10 weeks to 6-month-old male obese Zucker rats as a model of the metabolic syndrome. RANTES and MCP-1 serum levels are increased in obese vs lean Zucker rats and significantly reduced by long-term treatment with Rimonabant, which slowes weight gain in rats with the metabolic syndrome. Neutrophils and monocytes are significantly increased in young and old obese vs lean Zucker rats and lowered by Rimonabant. Platelet-bound fibrinogen is significantly enhanced in obese vs lean Zucker rats of both age, and is reduced by Rimonabant[1].
    Rimonabant (20 mg daily) exhibits a significant reduction in many cardiometabolic risk factors[4].

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

    Molecular Weight

    500.25

    Formula

    C22H22Cl4N4O

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    ClC1=CC=C(C2=C(C)C(C(NN3CCCCC3)=O)=NN2C4=CC=C(Cl)C=C4Cl)C=C1.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 33.33 mg/mL (66.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.9990 mL 9.9950 mL 19.9900 mL
    5 mM 0.3998 mL 1.9990 mL 3.9980 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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 (5.00 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      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.
    • Protocol 2

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

      Solubility: ≥ 2.5 mg/mL (5.00 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

    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, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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

    Purity: 99.79%

    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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9990 mL 9.9950 mL 19.9900 mL 49.9750 mL
    5 mM 0.3998 mL 1.9990 mL 3.9980 mL 9.9950 mL
    10 mM 0.1999 mL 0.9995 mL 1.9990 mL 4.9975 mL
    15 mM 0.1333 mL 0.6663 mL 1.3327 mL 3.3317 mL
    20 mM 0.1000 mL 0.4998 mL 0.9995 mL 2.4988 mL
    25 mM 0.0800 mL 0.3998 mL 0.7996 mL 1.9990 mL
    30 mM 0.0666 mL 0.3332 mL 0.6663 mL 1.6658 mL
    40 mM 0.0500 mL 0.2499 mL 0.4998 mL 1.2494 mL
    50 mM 0.0400 mL 0.1999 mL 0.3998 mL 0.9995 mL
    60 mM 0.0333 mL 0.1666 mL 0.3332 mL 0.8329 mL
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Product Name:
    Rimonabant Hydrochloride
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