Art. -Nr.: HY-14136

Rimonabant

Name: Rimonabant
Brand: MedChemExpress
SKU: HY-14136
Price: 32.00 USD
Availability: InStock
Rating: 5 (16 reviews)

(Synonyms: SR141716)

16 Cited Publications

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Based on 16 publication(s) in Google Scholar

Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a K_i of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).

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Reinheit : 99.52%
CAS. Nr.: 168273-06-1
Formel: C₂₂H₂₁Cl₃N₄O
Molecular Weight:463.79

Speicherung:

4°C, sealed storage, away from moisture

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

Rimonabant Chemical Structure

CAS. Nr.: 168273-06-1

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

CB1

1.8 nM (Ki)

Alle Cannabinoid Receptor Isoform-spezifische Produkte anzeigen :

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	6 nM Compound: 1	Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells Inhibitory concentration against human recombinant cannabinoid receptor type 1 expressed in Chinese Hamster Ovary (CHO) cells	[PMID: 15713403]
CHO	IC₅₀	6.1 nM Compound: SR-141716	Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells Inhibition of [3H]CP-55940 binding to human recombinant CB1 receptor in CHO cells	[PMID: 17181138]
CHO	IC₅₀	600 nM Compound: SR-141716	Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells Inhibition of [3H]CP-55940 binding to human recombinant CB2 receptor in CHO cells	[PMID: 17181138]
CHO	IC₅₀	6.1 nM Compound: 1	Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells	[PMID: 17293109]
CHO	IC₅₀	603.3 nM Compound: 1	Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in CHO cells	[PMID: 17293109]
CHO	IC₅₀	1760 nM Compound: rimonabant	Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells Displacement of [3H]WIN-55212-2 from human cannabinoid CB2 receptor expressed in CHO cells	[PMID: 18337096]
CHO	IC₅₀	1760 nM Compound: rimonabant, SR-141716	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHO cells	[PMID: 19022666]
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	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	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	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	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	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	IC₅₀	51 nM Compound: Rimonabant	Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level Inverse agonist activity against CB1 receptor expressed in human CHO cells assessed as effect on forskolin-stimulated cAMP level	[PMID: 22959249]
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	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	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	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	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	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	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	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	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-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, SR-141716,rimonabant	Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells Displacement of [3H]WIN-55212-2 from human CB2 receptor expressed in CHOK1 cells	[PMID: 18243711]
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	>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	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	EC₅₀	0.24 μM Compound: 1	Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity Antagonist activity at human cannabinoid CB1 receptor expressed in CHOK1 cells assessed as cAMP activity	[PMID: 19328683]
CHO-K1	EC₅₀	31.21 μM Compound: 1	Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity Antagonist activity at human cannabinoid CB2 receptor expressed in CHOK1 cells assessed as cAMP activity	[PMID: 19328683]
CHO-K1	IC₅₀	1760 nM Compound: Rimonabant	Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells Displacement of [3H]WIN-552122 from human CB2 receptor expressed in CHOK1 cells	[PMID: 19850473]
CHO-K1	IC₅₀	4.5 nM Compound: Rimonabant	Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding Antagonist activity at human recombinant CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-stimulated GTPgammaS binding	[PMID: 19954978]
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]
CHO-K1	IC₅₀	4.5 nM Compound: Rimonabant	Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding Antagonist activity at human CB1 receptor expressed in CHO-K1 cells assessed as inhibition of CP-55940-induced GTPgammaS binding	[PMID: 20015647]
CHO-K1	IC₅₀	1760 nM Compound: 1	Displacement of [3H]WIN-55212-2 from human recombinant CB2 receptor expressed in CHO-K1 cell membrane Displacement of [3H]WIN-55212-2 from human recombinant CB2 receptor expressed in CHO-K1 cell membrane	[PMID: 20045337]
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]
COS-7	IC₅₀	5.1 nM Compound: Rimonabant	Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells Displacement of [3H]CP-55940 from human CB1 receptor expressed in COS7 cells	[PMID: 20015647]
HEK293	EC₅₀	18.2 nM Compound: 1, rimonabant, SR-141716A	Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding	[PMID: 18712856]
HEK293	IC₅₀	15 nM Compound: 1, rimonabant, SR-141716A	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells	[PMID: 18712856]
HEK293	IC₅₀	1939.8 nM Compound: 1, rimonabant, SR-141716A	Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells	[PMID: 18712856]
HEK293	EC₅₀	18.2 nM Compound: SR-141716A	Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding Antagonist activity at human CB1 receptor expressed in HEK293 cells assessed as inhibition of Eu-GTP binding	[PMID: 19095444]
HEK293	IC₅₀	1.9 nM Compound: SR-141716A	Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells Displacement of [3H]CP-55940 from human CB2 receptor expressed in HEK293 cells	[PMID: 19095444]
HEK293	IC₅₀	15 nM Compound: SR-141716A	Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells Displacement of [3H]CP-55940 from human CB1 receptor expressed in HEK293 cells	[PMID: 19095444]
HEK293	EC₅₀	15.7 nM Compound: 1, SR-141716A	Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding Inverse agonist activity at human recombinant CB1R expressed in HEK293 cells assessed as inhibition of CP-55940-stimulated Eu-GTP binding	[PMID: 19530697]
HEK293	IC₅₀	13.2 nM Compound: 1, SR-141716A	Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells Displacement of [3H]CP-55940 from human recombinant CB1R expressed in HEK293 cells	[PMID: 19530697]
HEK293	IC₅₀	1631.1 nM Compound: 1, SR-141716A	Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells Displacement of [3H]CP-55940 from human recombinant CB2R expressed in HEK293 cells	[PMID: 19530697]
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	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	2.8 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	IC₅₀	1.35 nM Compound: 1, SR-141716A, rimonabant	Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level Inverse agonist at human CB1 receptor expressed in SF9 cells assessed as decrease in GTPgammaS level	[PMID: 18448340]
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. Further protocols information, click here.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 168273-06-1
Appearance Solid
Molecular Weight 463.79
Formel C₂₂H₂₁Cl₃N₄O
Color White to off-white
SMILES

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

SR141716
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

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

Publications (16)

All In Vivo Efficacy StudyBio/Physico-chemical AssayCell Proliferation/Viability Assay

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Journal Impact Factor

Cell

In vivo transcriptomic, functional, circuit-based, and translational analyses of enteric neurons. [Abstract]

2025 Dec 24;188(26):7547-7570.e45 PMID: 41406962

Rimonabant 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).
Cell

Crystal Structures of Membrane Transporter MmpL3, an Anti-TB Drug Target. [Abstract]

2019 Jan 24;176(3):636-648.e13. PMID: 30682372

Rimonabant 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 (K_d value) of 29 μM.
Autophagy

Cannabidiol inhibits human glioma by induction of lethal mitophagy through activating TRPV4. [Abstract]

2021 Nov;17(11):3592-3606. PMID: 33629929

Rimonabant 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.
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Int J Mol Sci

Genetically Encoded CB2R-Based Fluorescent Sensor Enables Rapid Screening and Functional Assessment of Cannabinoid Modulators. [Abstract]

2026 Feb 24;27(5):2095. PMID: 41828327
Int J Mol Sci

Assessment of Abuse Potential of Three Indazole-Carboxamide Synthetic Cannabinoids 5F-ADB, MDMB-4en-PINACA and ADB-4en-PINACA. [Abstract]

2025 Jul 3;26(13):6409. PMID: 40650186
Int J Mol Sci

Pharmacological Evaluation of Cannabinoid Receptor Modulators Using GRABeCB2.0 Sensor. [Abstract]

2024 May 3;25(9):5012. PMID: 38732230

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

Fluorescent signal of Rimonabant at inhibiting GRAB_eCB2.0 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 GRAB_eCB2.0 sensor, indicating inverse agonist activity (EC₅₀= 42 nM).
J Psychopharmacol

"Modulatory role of baseline impulsivity on the acute and persistent effects of CB1 agonism on impulsive choice". [Abstract]

2025 Jul 31:2698811251355603. PMID: 40741841

Rimonabant 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 AUC_log in rats via antagonism of the CB1 receptor.
ACS Omega

Receptor-Selective Modulation of Cannabinoid Signaling by Cardamonin: Integrating Molecular Dynamics, Free Energy Calculations, and Behavioral Validation. [Abstract]

2026 Apr 13;11(16):23820-23832. PMID: 42077871
Molecules

BI-5756 Reduces Graft-Versus-Host Disease Through CB1-Mediated Treg Upregulation. [Abstract]

2025 Aug 28;30(17):3517. PMID: 40942043
Sci Rep

Hyperuricemia aggravates acute pancreatitis through CNR1-mediated inflammatory signaling and gut-pancreas axis dysregulation: a multi-omics and clinical study. [Abstract]

2026 Jun 4. PMID: 42243316
Cancers (Basel)

Assessment of Cannabidiol and Δ9-Tetrahydrocannabiol in Mouse Models of Medulloblastoma and Ependymoma. [Abstract]

2021 Jan 18;13(2):330. PMID: 33477420
J Gerontol A Biol Sci Med Sci

Rimonabant treatment partly attenuates skeletal muscle loss following immobilization in young and in old, sarcopenic male mice. [Abstract]

2025 Aug 28:glaf189. PMID: 40875529
Structure

Structure-based design of anti-mycobacterial drug leads that target the mycolic acid transporter MmpL3. [Abstract]

2022 Oct 6;30(10):1395-1402.e4. PMID: 35981536
Neuroscience

Divergent Response to Cannabinoid Receptor Stimulation in High and Low Stress-Induced Analgesia Mouse Lines Is Associated with Differential G-Protein Activation. [Abstract]

2019 Apr 15:404:246-258. PMID: 30794845
Tissue Cell

Integrated network pharmacology and experimental validation to elucidate the mechanism of WIN55,212-2 in mitigating sepsis-induced pulmonary fibrosis in mice. [Abstract]

2026 May 25:102:103638. PMID: 42202462

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (215.61 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

2.1561 mL

10.7807 mL

21.5615 mL

5 mM

0.4312 mL

2.1561 mL

4.3123 mL

10 mM

0.2156 mL

1.0781 mL

2.1561 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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

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 90% Corn Oil

Solubility: ≥ 5 mg/mL (10.78 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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

Protokoll

All Molecular Biology

Membrane Protein Extraction Using Detergents and Chaotropes
Membrane protein extraction with detergents and chaotropes solubilizes lipid-bilayer-associated proteins by disrupting protein-lipid and protein-protein interactions while maintaining proteins in a soluble state for downstream electrophoresis, purification, or mass spectrometry. Chaotropes such as urea and thiourea improve solubilization of difficult proteins, while nonionic and zwitterionic detergents such as CHAPS, ASB-14, SB 3-10, MEGA-10, dodecyl maltoside, and Triton X-100 differ in extraction efficiency depending on sample type and membrane protein properties.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (480 KB)
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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)
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Handling Instructions (2659 KB)

Verweise

[1]. Seely KA, Brents LK, Franks LN, Rajasekaran M, Zimmerman SM, Fantegrossi WE, Prather PL. AM-251 and rimonabant act as direct antagonists at mu-opioid receptors: Implications for opioid/cannabinoid interaction studies. Neuropharmacology. 2012 Oct;63(5):9 [Content Brief]

[2]. Leite, C.E., et al. Rimonabant: An antagonist drug of the endocannabinoid system for the treatment of obesity. Pharmacol Rep 61 217-224 (2009).

[3]. 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]

[4]. 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]

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	2.1561 mL	10.7807 mL	21.5615 mL	53.9037 mL
	5 mM	0.4312 mL	2.1561 mL	4.3123 mL	10.7807 mL
	10 mM	0.2156 mL	1.0781 mL	2.1561 mL	5.3904 mL
	15 mM	0.1437 mL	0.7187 mL	1.4374 mL	3.5936 mL
	20 mM	0.1078 mL	0.5390 mL	1.0781 mL	2.6952 mL
	25 mM	0.0862 mL	0.4312 mL	0.8625 mL	2.1561 mL
	30 mM	0.0719 mL	0.3594 mL	0.7187 mL	1.7968 mL
	40 mM	0.0539 mL	0.2695 mL	0.5390 mL	1.3476 mL
	50 mM	0.0431 mL	0.2156 mL	0.4312 mL	1.0781 mL
	60 mM	0.0359 mL	0.1797 mL	0.3594 mL	0.8984 mL
	80 mM	0.0270 mL	0.1348 mL	0.2695 mL	0.6738 mL
	100 mM	0.0216 mL	0.1078 mL	0.2156 mL	0.5390 mL

Bioz

Keywords

Rimonabant

16 Cited Publications

100 mg Angebot einholen

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Rimonabant

Publications Citing Use of MedChemExpress (MCE) Rimonabant

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