AM251

Catalog No.S2819

AM251 Chemical Structure

Molecular Weight(MW): 555.24

AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.

Size Price Stock Quantity  
In DMSO USD 160 In stock
USD 70 In stock
USD 110 In stock
USD 370 In stock
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Cited by 2 Publications

2 Customer Reviews

  • 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

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Biological Activity

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.
Targets
CB1 [2]
In vitro

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. [1] AM251 reduces cholesteryl ester synthesis in unstimulated and acetylated LDL-stimulated Raw 264.7 macrophages, CB2+/+ and CB2 −/− peritoneal macrophages. [2]

In vivo AM251 causes a sustained reduction of daily food intake in the rat. [3] AM251 produces food avoidance and behaviors associated with nausea but does not impair feeding efficiency in rats. [4] AM251 disrupts memory consolidation of the inhibitory avoidance task. [5] 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. [6] AM251 (4.0 mg/kg) reduces freezing during a conditioned tone cue played within a novel context. [7]

Protocol

Animal Research:[5]
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  • Animal Models: Moderately obese male Lewis rats
  • Formulation: 2% dimethyl sulfoxide,1% Tween 80 and 97% physiological saline
  • Dosages: 1.25 mg/kg, 2.5 mg/kg and 5 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 40 mg/mL (72.04 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing.
8 mg/mL

* 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.

Chemical Information

Molecular Weight 555.24
Formula

C22H21Cl2IN4O

CAS No. 183232-66-8
Storage powder
in solvent
Synonyms N/A

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Tech Support

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.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID