Rimonabant
Based on 14 publication(s) in Google Scholar
Rimonabant (SR141716) is a highly potent, brain penetrated and selective central cannabinoid receptor (CB1) antagonist with a Ki of 1.8 nM. Rimonabant (SR141716) also inhibits Mycobacterial membrane protein Large 3 (MMPL3).
For research use only. We do not sell to patients.
- Purity: 99.52%
- CAS No.: 168273-06-1
- Formula: C22H21Cl3N4O
- Molecular Weight:463.79
-
Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications Citing Use of MedChemExpress (MCE) Rimonabant
More- Cell. 2025 Dec 24;188(26):7547-7570.e45 [Abstract]
- Cell. 2019 Jan 24;176(3):636-648.e13. [Abstract]
- Autophagy. 2021 Nov;17(11):3592-3606. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- J Psychopharmacol. 2025 Jul 31:2698811251355603. [Abstract]
- Int J Mol Sci. 2026 Feb 24;27(5):2095. [Abstract]
- Int J Mol Sci. 2025 Jul 3;26(13):6409. [Abstract]
- Int J Mol Sci. 2024 May 3;25(9):5012. [Abstract]
- Molecules. 2025 Aug 28;30(17):3517. [Abstract]
- Cancers (Basel). 2021 Jan 18;13(2):330. [Abstract]
- ACS Omega. 2026 Apr 13;11(16):23820-23832. [Abstract]
- Structure. 2022 Oct 6;30(10):1395-1402.e4. [Abstract]
- J Gerontol A Biol Sci Med Sci. 2025 Aug 28:glaf189. [Abstract]
- Neuroscience. 2019 Apr 15:404:246-258. [Abstract]
-
In Vivo Efficacy Study
-
In Vivo Efficacy Study
-
Bio/Physico-chemical Assay
-
Cell Proliferation/Viability Assay
-
Bio/Physico-chemical Assay
Biological Activity
|
CB1 1.8 nM (Ki) |
|
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] |
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 168273-06-1
-
Appearance Solid
-
Molecular Weight 463.79
-
Formula 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
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (14)
-
Journal Impact Factor
-
Most Recent
-
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
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 (Kd 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 -
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 AUClog in rats via antagonism of the CB1 receptor.
-
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
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 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).
-
Molecules
2025 Aug 28;30(17):3517. PMID: 40942043 -
Cancers (Basel)
Assessment of Cannabidiol and Δ9-Tetrahydrocannabiol in Mouse Models of Medulloblastoma and Ependymoma. [Abstract]2021 Jan 18;13(2):330. PMID: 33477420 -
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 -
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 -
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 -
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
Solvent & Solubility
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)
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.
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.
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.
Please enter the basic information of animal 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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Purity & Documentation
-
Data Sheet (279 KB)
-
SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
-
Handling Instructions (2659 KB)
References
[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]
[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]
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 (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.
| 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 |