For research use only.
CAS No. 183232-66-8
AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
Selleck's AM251 has been cited by 8 publications
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Inhibition of CB1 suppresses the proliferation and migration and induces apoptosis of RCC cells. a Western blot analysis of CB1 protein in RCC cell lines (786-O, CAKI-1, CAKI-2, 769-P, A498, and ACHN) and normal cell line HK-2, and β-actin was used as a loading control for western blot assays. b RCC cell lines were treated at the indicated concentrations for different time points, and the cell viability was analyzed by MTT assay. AM251-induced cell death in 769-P cells in a dose- and time-dependent manner. c AM251-induced cell death in 786-O cells in a dose- and timedependent manner. d AM251 reduced migration in 786-O and 769-P cell lines at 20 and 30 μM concentrations. e The transmembrane cell number of 786-O and 769-P cells after treatment with different concentrations of AM251 significantly decreased compared with untreated control.
Tumour Biol, 2016, DOI: 10.1007/s13277-016-5447-6. AM251 purchased from Selleck.
Effect of AM251 treatment on the CORT response to stress. Group-housed and socially isolated rats were intraperitoneally injected with AM251 or vehicle 30 min before exposure to foot-shock stress, and were sacrificed 30 min thereafter. Non-shocked controls were sacrificed 60 min after injection. Data are mean ± SEM of values from 10 rats per group and are expressed as ng/ml of plasma. Data were analyzed by three-way ANOVA (housing × drug treatment × stress conditions) followed by Newman-Keuls post-hoc test. ap<0.01 vs. the respective non-shocked controls; bp < 0.01 vs. group-housed vehicle-treated rats; cp < 0.01 vs. group-housed vehicle-treated + foot-shock rats.
Neuropharmacology, 2018, 133:242-253. AM251 purchased from Selleck.
Purity & Quality Control
Choose Selective Cannabinoid Receptor Inhibitors
|Description||AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.|
|Features||A selective cannabinoid 1 blocker.|
AM251 reduces veratridine-dependent (tetrodotoxin suppressible) release of L-glutamic acid and GABA from synaptosomes with IC50 of 8.5 μM and 9.2 μM, respectively. AM251 increases (by 2.3 times) the Kd of radioligand without altering Bmax. AM251 inhibits equilibrium binding by allosterically accelerating the dissociation of the [3H]-batrachotoxinin A 20-alpha-benzoate:sodium channel complex.  AM251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2+/+ and CB2 −/− peritoneal macrophages. 
|In vivo||AM251 causes a sustained reduction of daily food intake in the rat.  AM251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats.  AM251 disrupts memory consolidation of the inhibitory avoidance task.  AM251 has caused a significative decrease in the test step-down latency when compared to the control group, but no differences are detected in the open field habituation task, including the number of crossings, i.e. there are no motor effects.  AM251 (4.0 mg/kg) reduces freezing during a conditioned tone cue played within a novel context. |
-  Liao C, et al. Basic Clin Pharmacol Toxicol, 2004, 94(2), 73-78.
-  Thewke D, et al. Biochem Biophys Res Commun, 2009, 381(2), 181-186.
-  Chambers AP, et al. Physiol Behav, 2004, 82(5), 863-869.
|In vitro||DMSO||40 mg/mL (72.04 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50% ddH2O
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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