Rimonabant Hydrochloride (Synonyms: SR 141716A Hydrochloride)

Name: Rimonabant Hydrochloride
Brand: MedChemExpress
SKU: HY-14137
Rating: 5.0 (6 reviews)

Cat. No.: HY-14137 Purity: 99.95%: FAQs
Data Sheet SDS COA Handling Instructions

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Rimonabant Hydrochloride (SR 141716A Hydrochloride) is a highly potent and selective central cannabinoid receptor (CB1) antagonist with an K_i 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.

Rimonabant Hydrochloride Chemical Structure

CAS No. : 158681-13-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
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Based on 6 publication(s) in Google Scholar

Other Forms of Rimonabant Hydrochloride:

Rimonabant-d₁₀ hydrochloride Get quote
Rimonabant Get quote
Rimonabant (Hydrochloride) (Standard) Get quote

6 Publications Citing Use of MCE Rimonabant Hydrochloride

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CB1 CB2

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

CB1

1.8 nM (Ki)

Cellular Effect

Cell Line	Type	Value	Description	References
BV-2	IC₅₀	16.17 μM Compound: Rimonabant	Inhibition of LPS-induced NO production in mouse BV-2 cells incubated for 24 hrs by Griess reagent based method Inhibition of LPS-induced NO production in mouse BV-2 cells incubated for 24 hrs by Griess reagent based method	[PMID: 36371018]
CHO	IC₅₀	0.004 μM Compound: Rimonabant	Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay Antagonist activity at CB1 receptor transfected in CHO cells expressing apoaequorin as a reporter for G-protein-coupled receptor-mediated calcium signaling by bioluminescence assay	[PMID: 21376588]
CHO	IC₅₀	0.0135 μM Compound: 2, SR141716A	Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay Antagonist activity against CB1R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay	[PMID: 26151231]
CHO	EC₅₀	0.11 nM Compound: Rimonabant	Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins Inverse agonist activity at human cannabinoid CB1 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation after 60 mins	[PMID: 20047779]
CHO	IC₅₀	1.98 μM Compound: 1	Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting Displacement of [3H]CP55940 from human cannabinoid CB2 receptor expressed in CHO cells at pH 7.4 after 1 hr by liquid scintillation counting	[PMID: 21741835]
CHO	EC₅₀	10.1 μM Compound: 5	Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method Agonist activity at human GPR18 expressed in CHO cells assessed as induction of beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method	10.1039/C3MD00394A
CHO	IC₅₀	10.1 μM Compound: 1	Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay Antagonist activity at human GPR18 transfected in CHO cells assessed as delta9-THC-induced beta-arrestin recruitment incubated 60 mins prior to delta9-THC addition by beta-arrestin translocation assay	[PMID: 23679955]
CHO	IC₅₀	108 nM Compound: 1	Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay Inverse agonist activity at human recombinant CB1 receptor expressed in CHO cells by luciferase reporter gene assay	[PMID: 20045337]
CHO	IC₅₀	13 nM Compound: SR141716A, Rimonabant	Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay Antagonist activity at human CB1 receptor stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay	[PMID: 24445310]
CHO	EC₅₀	2.01 μM Compound: 6	Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay Agonist activity at GPR55 (unknown origin) expressed in CHO cells assessed as inhibition of LPI-induced beta-arrestin translocation after 90 mins by luminescence assay	[PMID: 24900561]
CHO	EC₅₀	2.01 μM Compound: 5	Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method Agonist activity at human GPR55 expressed in CHO cells assessed as induction of LPI-induced beta-arrestin recruitment by beta-galactosidase enzyme fragment complementation method	10.1039/C3MD00394A
CHO	IC₅₀	3.2 nM Compound: Rimonabant	Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader Antagonist activity at human cannabinoid CB1 receptor expressed in CHO cells coexpressing Galpha15/16 assessed as inhibition of CP-55940-induced Ca2+ release after 10 mins by micro plate reader	[PMID: 20047779]
CHO	EC₅₀	5 nM Compound: 1; SR141716A	Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay Inverse agonist activity at human CB1 receptor expressed in CHO cells assessed as increase in intracellular calcium mobilization after 90 secs by Calcein-4 AM-staining based FLIPR assay	[PMID: 26827137]
CHO	IC₅₀	9.1 μM Compound: 2, SR141716A	Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay Antagonist activity against CB2R (unknown origin) CHO cells stably expressing Galpha16 assessed as inhibition of CP55940-induced increase in intracellular calcium level pre-treated 10 mins before CP55940 stimulation by microplate reader based assay	[PMID: 26151231]
CHO	IC₅₀	92.5 nM Compound: Rimonabant	Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay Binding affinity to human CB2 receptor expressed in CHO cells by luciferase reporter gene assay	[PMID: 19850473]
CHO	IC₅₀	9800 nM Compound: SR141716A, Rimonabant	Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay Antagonist activity at CB2 receptor (unknown origin) stably expressed in CHO cells co-expressing co-expressing Ga15/16 assessed as calcium current after 45 mins by fluo-4 AM assay	[PMID: 24445310]
CHO-K1	IC₅₀	> 1000 nM Compound: Rimonabant	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells by liquid scintillation counting Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells by liquid scintillation counting	[PMID: 19128970]
CHO-K1	IC₅₀	120 nM Compound: 1, SR-141716,rimonabant	Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay Antagonist activity at human CB1 receptor expressed in CHOK1 cells by luciferase assay	[PMID: 18243711]
CHO-K1	IC₅₀	1760 nM Compound: 1	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO-K1 cells after 1 hr by liquid scintillation counting	[PMID: 20673729]
CHO-K1	IC₅₀	1760 nM Compound: SR-141716	Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry Displacement of [3H]WIN-55212-2 from human recombinant cannabinoid CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry	[PMID: 19269817]
CHO-K1	IC₅₀	1760 nM Compound: 1, rimonabant, SR-141716	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells by liquid scintillation spectrometry	[PMID: 18954042]
CHO-K1	IC₅₀	2.9 nM Compound: Rimonabant	Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay Inverse agonist activity at human CB1 receptor expressed in CHO-K1 cells by GTPgammaS binding assay	[PMID: 20015647]
HEK293	EC₅₀	1.5 nM Compound: 1, SR141716A, Zimulti	Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis Antagonist activity at human CB1 receptor overexpressed in HEK cells assessed as [35S]GTPgamma binding after 1 hr by liquid scintillation counting analysis	[PMID: 24175572]
HEK293	IC₅₀	2.79 μM Compound: 1	Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay Inhibition of human ERG expressed in HEK293 cells assessed as inhibition of potassium channel current after 5 mins by patch clamp assay	[PMID: 21741835]
HEK293	IC₅₀	2.8 nM Compound: SR141716	Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method Inverse agonist activity at human CB1 receptor expressed in HEK293 cell membranes assessed as suppression of [35S]GTPgammaS binding incubated for 60 mins by scintillation counting method	[PMID: 31596583]
HEK293-EBNA	EC₅₀	4 nM Compound: 1, rimonabant	Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay Inverse agonist activity at human CB1 receptor expressed in HEK293 EBNA cells by [35S]GTPgammaS incorporation assay	[PMID: 18083560]
Sf9	EC₅₀	0.05 μM Compound: Rimonabant	Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay Inverse agonist activity at human CB1 receptor expressed in Sf9 cells coexpressing Gbeta1gamma2 and RSG4 assessed as degradation of [gamma-33P]GTP after 20 mins by steady-state GTPase assay	[PMID: 25096297]

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.

Clinical Trial

Molecular Weight

500.25

Formula

C₂₂H₂₂Cl₄N₄O

CAS No.

158681-13-1

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
10 mM	0.1999 mL	0.9995 mL	1.9990 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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)

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: 99.95%

Select Batch:

Data Sheet (279 KB) SDS (420 KB)

COA (254 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Seely KA, et al. AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction studies. Neuropharmacology. 2012 Oct;63(5):905-15. [Content Brief]

[2]. Zhang B, et al. Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target. Cell. 2019 Jan 24;176(3):636-648.e13. [Content Brief]

[3]. Erdozain, A. M. et al. The inverse agonist effect of rimonabant on G protein activation is not mediated by the cannabinoid CB1 receptor: Evidence from postmortem human brain Biochemical Pharmacology (2012), 83(2), 260-268. [Content Brief]

Animal Administration

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

References

[1]. Seely KA, et al. AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction studies. Neuropharmacology. 2012 Oct;63(5):905-15. [Content Brief]

[2]. Zhang B, et al. Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target. Cell. 2019 Jan 24;176(3):636-648.e13. [Content Brief]

[3]. Erdozain, A. M. et al. The inverse agonist effect of rimonabant on G protein activation is not mediated by the cannabinoid CB1 receptor: Evidence from postmortem human brain Biochemical Pharmacology (2012), 83(2), 260-268. [Content Brief]

Complete Stock Solution Preparation Table

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

Rimonabant Hydrochloride Related Classifications

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.

Keywords:

Rimonabant158681-13-1SR 141716ACannabinoid ReceptorBacterialInhibitorinhibitorinhibit

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Rimonabant Hydrochloride (Synonyms: SR 141716A Hydrochloride)

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Other Forms of Rimonabant Hydrochloride:

Rimonabant Hydrochloride Related Antibodies

6 Publications Citing Use of MCE Rimonabant Hydrochloride

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•Related Screening Libraries:

•Related Small Molecules:

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View All Cannabinoid Receptor Isoform Specific Products:

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Purity & Documentation

References

Customer Review

Rimonabant Hydrochloride Related Antibodies

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Complete Stock Solution Preparation Table

Rimonabant Hydrochloride Related Classifications

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