Rimonabant hydrochloride

SKU: orb1308356

Description

Rimonabant hydrochloride (SR 141716A) is a selective, high-affinity antagonist of the central cannabinoid CB1 receptor. It is widely used in metabolic and obesity research to investigate the endocannabinoid system's role in appetite and energy balance, both in vitro and in vivo.

Research Area

Infectious Disease & Virology, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	158681-13-1
MW	500.25
Purity	>99.99% (May vary between batches)
Formula	C₂₂H₂₂Cl₄N₄O
SMILES	n1(nc(c(c1c1ccc(cc1)Cl)C)C(=O)NN1CCCCC1)c1c(cc(cc1)Cl)Cl.Cl
Target	Antibacterial,Cannabinoid Receptor
Solubility	10% DMSO+90% Corn Oil:2.5 mg/mL (5 mM);DMSO:60 mg/mL (119.94 mM)

Bioactivity

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Target IC50	CB1 receptor:1.8 nM(ki)
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. 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. Read more...
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. 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). Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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inhibit, Inhibitor, Bacterial, CB1, CB, Cannabinoid Receptor, CannabinoidReceptor, SR 141716A, SR 151716A, Rimonabant, Rimonabant hydrochloride, Rimonabant Hydrochloride

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Compound Identifiers

PubChem CID

104849 ↗

Key Properties

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No computed properties available.

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