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Rimonabant hydrochloride

Catalog No. T1519   CAS 158681-13-1
Synonyms: SR 151716A, SR 141716A

Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.

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Rimonabant hydrochloride Chemical Structure
Rimonabant hydrochloride, CAS 158681-13-1
Pack Size Availability Price/USD Quantity
5 mg In stock $ 38.00
10 mg In stock $ 61.00
25 mg In stock $ 118.00
50 mg In stock $ 217.00
100 mg In stock $ 327.00
500 mg In stock $ 783.00
1 mL * 10 mM (in DMSO) In stock $ 68.00
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Purity: 100%
Purity: 99.5%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Rimonabant hydrochloride (SR 141716A) is a cannabinoid receptor antagonist, binding selectively to central cannabinoid receptors (CB1) with high affinity.
Targets&IC50 CB1 receptor:1.8 nM(ki)
In vitro Rimonabant hydrochloride (SR 141716A) binds selectively to central cannabinoid receptors (CB1) with high affinity (Ki=2 nM), and blocks the inhibitory effects of cannabinoid receptor agonists in the mouse vas deferens, dopamine-stimulated adenylyl cyclase and WIN 55212-stimulated GTPγS binding[1]. Rimonabant dose-dependently inhibited CO synthesis in Raw 264.7 macrophages, with 1 μM producing a significant (~40%) decrease compared to untreated controls and concentrations ≥ 5 μM producing near complete inhibition. A small, but significant, reduction of TG and DG synthesis is also observed with Rimonabant at concentrations ≥ 10 μM. Inhibition of CO synthesis in Raw 264.7 macrophages by Rimonabant (IC50 value 2.9±0.38 μM) is very similar to that of AM251 and SR144528 (IC50 value 2.6±0.26 μM and 2.5±0.32 μM, respectively), two related compounds previously demonstrated to be potent ACAT inhibitors. Mouse peritoneal macrophages also displayed significantly reduced CO synthesis in response to Rimonabant treatment. Rimonabant at concentrations ≥ 1 μM significantly inhibits CO synthesis in CHO-ACAT1 and CHO-ACAT2 cells in a concentration-dependent manner with similar efficiency (IC50s of 1.5±1.2 μM and 2.2±1.1 μM, respectively)[2].
In vivo Pretreatment with Rimonabant hydrochloride (SR 141716A) blocks the antinociceptive, discriminative stimulus, memory impairing and hypolocomotor effects produced by Δ-9-THC. SR 141716A also precipitates a withdrawal syndrome in rats treated chronically with Δ-9-THC[1]. Pretreatment of mice with 0.1?mg/kg of WIN 55212-2 is effective in increasing the CPP induced by MDMA , while 1?mg/kg of Rimonabant specifically blocks CB1 receptors and does not act as an inverse agonist[3].
Kinase Assay Raw 264.7 cells (2×106/well) in 12-well plates are rinsed with PBS and refed culture media supplemented with varying amounts of Rimonabant 1h prior to supplementation with 7-ketocholesterol (7KC). All wells are adjusted to receive equal amounts of vehicle. Following a 16 h incubation, caspase-3 and caspase 3-like activity is determined[2].
Synonyms SR 151716A, SR 141716A
Molecular Weight 500.25
Formula C22H22Cl4N4O
CAS No. 158681-13-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL(100 mM)

TargetMolReferences and Literature

1. Vivian JA, et al. Analgesic, respiratory and heart rate effects of cannabinoid and opioid agonists in rhesus monkeys: antagonist effects of SR 141716A. J Pharmacol Exp Ther. 1998 Aug;286(2):697-703. 2. Netherland C, et al. Rimonabant is a dual inhibitor of acyl CoA:cholesterol acyltransferases 1 and 2. Biochem Biophys Res Commun. 2010 Aug 6;398(4):671-6. 3. Rodríguez-Arias, M., Roger-Sánchez, C., Vilanova, I., Revert, N., Manzanedo, C., Miñarro, J., & Aguilar, M. (2016). Effects of Cannabinoid Exposure during Adolescence on the Conditioned Rewarding Effects of WIN 55212-2 and Cocaine in Mice: Influence of the Novelty-Seeking Trait. Neural Plasticity, 2016, 1-11. doi: 10.1155/2016/6481862

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Approved Drug Library Inhibitor Library GPCR Compound Library EMA Approved Drug Library Anti-Cancer Drug Library Drug Repurposing Compound Library Bioactive Compounds Library Max Anti-Infection Compound Library Approved Drug Library Anti-Obesity Compound Library

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Keywords

Rimonabant hydrochloride 158681-13-1 GPCR/G Protein Microbiology/Virology Antibacterial Cannabinoid Receptor Rimonabant Bacterial Rimonabant Hydrochloride Inhibitor SR 151716A SR 141716A inhibit inhibitor

 

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